TW201018400A - Liquid aqueous plant protection formulations - Google Patents
Liquid aqueous plant protection formulations Download PDFInfo
- Publication number
- TW201018400A TW201018400A TW098134177A TW98134177A TW201018400A TW 201018400 A TW201018400 A TW 201018400A TW 098134177 A TW098134177 A TW 098134177A TW 98134177 A TW98134177 A TW 98134177A TW 201018400 A TW201018400 A TW 201018400A
- Authority
- TW
- Taiwan
- Prior art keywords
- plant protection
- acid
- formulation
- weight
- solvent
- Prior art date
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- 239000000203 mixture Substances 0.000 title claims abstract description 200
- 238000009472 formulation Methods 0.000 title claims abstract description 161
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- 238000000034 method Methods 0.000 claims abstract description 18
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Classifications
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- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N25/00—Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application, e.g. seed treatment or sequential application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests
- A01N25/02—Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application, e.g. seed treatment or sequential application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests containing liquids as carriers, diluents or solvents
- A01N25/04—Dispersions, emulsions, suspoemulsions, suspension concentrates or gels
-
- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N25/00—Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application, e.g. seed treatment or sequential application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests
-
- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
- A01N43/64—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with three nitrogen atoms as the only ring hetero atoms
- A01N43/647—Triazoles; Hydrogenated triazoles
- A01N43/653—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
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- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N47/00—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a ring and having no bond to a carbon or hydrogen atom, e.g. derivatives of carbonic acid
- A01N47/08—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a ring and having no bond to a carbon or hydrogen atom, e.g. derivatives of carbonic acid the carbon atom having one or more single bonds to nitrogen atoms
- A01N47/10—Carbamic acid derivatives, i.e. containing the group —O—CO—N<; Thio analogues thereof
- A01N47/24—Carbamic acid derivatives, i.e. containing the group —O—CO—N<; Thio analogues thereof containing the groups, or; Thio analogues thereof
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- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N47/00—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a ring and having no bond to a carbon or hydrogen atom, e.g. derivatives of carbonic acid
- A01N47/08—Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a ring and having no bond to a carbon or hydrogen atom, e.g. derivatives of carbonic acid the carbon atom having one or more single bonds to nitrogen atoms
- A01N47/28—Ureas or thioureas containing the groups >N—CO—N< or >N—CS—N<
- A01N47/38—Ureas or thioureas containing the groups >N—CO—N< or >N—CS—N< containing the group >N—CO—N< where at least one nitrogen atom is part of a heterocyclic ring; Thio analogues thereof
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- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Health & Medical Sciences (AREA)
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- Agronomy & Crop Science (AREA)
- Pest Control & Pesticides (AREA)
- Plant Pathology (AREA)
- Engineering & Computer Science (AREA)
- Dentistry (AREA)
- Wood Science & Technology (AREA)
- Environmental Sciences (AREA)
- Toxicology (AREA)
- Dispersion Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Pretreatment Of Seeds And Plants (AREA)
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201018400 六、發明說明: 【發明所屬之技術領域】 本發明係關於一或多種植物保護劑之液態水性植物保護 調配物、該等植物保護調配物用於處理植物及種子之用 途、相應方法及經處理之種子。 【先前技術】 藉由施用適宜植物保護組合物來保護有用植物或農作物 植物免於被對植物有害之生物體侵襲、定向控制有用植物 之生長以及控制有害植物係提高產量且因此保證生產出安 全之基於植物之食品的重要手段。 許多植物(尤其有用植物)在萌芽及出苗之前及之後的階 段期間對植物致病真菌、細菌、病毒、線蟲及昆蟲之侵襲 極為敏感。此可能首先歸因於植物部分之尺寸較小,使得 植物難以彌補損傷。第二,植物之天然防禦機制在此早期 生長階段通常尚未形成。因此,在萌芽之前及期間對植物 實施保護係減少植物損傷之重要手段。 為防止種子及秧苗疾病,在播種之前用拌種產品對種子 進行處理,該等產品包含植物保護劑,通常為殺真菌劑, 且通常額外包含其他殺蟲劑(尤其殺昆蟲劑)。當前,有機 化學殺真菌劑及殺昆蟲劑大多以水性調配物形式使用以 確保與目標生物體充分相互作用。然而,許多該等活性物 質僅微溶於水或根本不溶於水’即其在25。〇下之水溶解度 小於5 g/l,通常小於1 g/l且尤其小於〇 ! g/1。因此製備 可容易地用水稀釋之殺蟲化合物之穩定調配物係重新提起 143575.doc 201018400 之問題。 除調配物之穩定性外,亦存在其他對種子處理應用極為 重要之因素。因此,在施用拌種產品後,種子應展示良好 机動性質,由此減少拌種過程期間或播種期間在機器中聚 ,集或結塊,以達到高通過率。而且,拌種產品低磨擦甚為 有利,此乃因此引起的拌種過程期間或播種期間形成之粉 塵減少能夠提高作業安全性及環境相容性。 ❹ < 拌種時,具有有限水溶解度之有機殺蟲劑通常調配成懸 浮濃縮物或可乳化濃縮物,以在用水稀釋後使用。 在可乳化濃縮物中,活性物質與表面活性物質一起以存 於有機水不混溶性溶劑(通常為烴混合物及/或脂肪酸甲基 知)中之溶液形式存在。缺點係使用大量通常具有毒性之 溶劑且稀釋後穩定性較差。 懸洋濃縮物係其中活性物質以小固體(例如精細研磨)顆 粒形式存在之調配物,該等小固體顆粒藉助表面活性物質 • 而懸浮於水性分散介質中。表面活性物質之任務係將活性 物質顆粒穩定於分散介質中。然而,使用懸浮濃縮物通常 會伴隨諸多問題,此係緣於如下事實:在長時間或高溫儲 存後顆粒會發生沉降且其再懸浮極為困難,且儲存期間會 形成結晶物質。因此,該等調配物難以處理,且其生物活 性可能不一致。而且,懸浮濃縮物限於相對較高熔點之活 性物質。而且,許多植物保護劑在調配成懸浮濃縮物時會 部分地被水「滅活」。 儘管基於水性懸浮濃縮物之市售拌種產品較可乳化濃縮 143575.doc 201018400 物更環保,但其不具有較佳施用特性。 仙Γ子'農縮物及可乳化濃縮物之—種替代係微乳液(me)。 微礼液在包含活性物質之微乳液情形下亦稱為細調配 物’其為由水及至少—種不與水混溶或僅與水略微混溶之 有機溶劑組成之液態多相系統,該等系統包含分散相及連 續相’分散相形成微滴或囊泡或其他能夠形成複合結構 者與a通礼液相比,微乳液中之平均相界距離(通常為 分散相之平均粒徑或微滴尺寸(z =藉由光散射測定之平均 直徑))至多為前者的1/5,且通常不大於500 nm,尤佳不大 於300 nm或甚至2〇〇 nm,而乳液中之微滴之平均直徑在 μηι範圍内。另一顯著特徵係微乳液在熱力學上較為穩定 且可在無礼液需要之高能量輸入下形成。由於分散相或複 合通道之粒杈(微滴尺寸)較小,因此微乳液在視覺上係透 明的。 有機殺蟲劑之微乳液調配物通常基於水,且額外包含至 少一種表面活性劑及至少一種助溶劑或助表面活性劑,其 通常為有機溶劑或低分子量聚伸烷基醚。由於高水含量, 故與可乳化濃縮物(EC)相比,使用ME調配物可降低諸如 可燃性、毒性、對環境造成負面影響等風險且降低成本。 由於包含活性物質之分散相之粒徑較小,因此在許多情形 下更可能達成高生物利用度。然而,難以調配微溶於水之 活性物質的微乳液而使其在微滴尺寸、均勻性及活性物質 結晶趨勢方面具有持久穩定性。而且,微滴尺寸應在甚至 用水稀釋後仍保持穩定’以保留獲自濃縮調配物之稀釋物 143575.doc 201018400 的生物活性。 包含疏水性農用化學品、烷酸烷基酯作為第一溶劑、多 元醇或多元醇縮合物作為第二溶劑及表面活性劑之微乳液 . 濃縮物係自EP 1 347 681獲知。該專利僅概括主張該等漢 、縮物在植物保護中之用途,而未闡述具體施用(例如用於 處理種子)。 WO 2006/030006闞述基於包含殺真菌劑護汰芬 • (flutriafol)、表面活性劑系統、防凍劑及水不溶性液 微乳液的拌種組合物,該水不溶性液體選自乳酸烷基酯及 己二酸、戊二酸及琥珀酸之二烷基酯。並未提及該狹窄範 圍以外的組合物。 自 W0 2.007/028382、WO 2007/028387及 WO 2007/028388 獲知三唑殺真菌劑之液態調配物,其含有植物油之酯、至 少一種水混溶性極性非質子助溶劑及至少一種水不混溶性 助溶劑。 φ 【發明内容】 因此,本發明之一目的係提供寬範圍活性物質均具有有 利種子處理特性之植物保護調配物。特定言之,意欲使其 • 因具有咼穩定性及均質活性物質分佈而與眾不同。另外, • 意欲使經該等調配物處理之種子具有良好流動性質且拌種 摩擦較低。 令人驚奇的是’該目的可藉由下文所述之液態水性植物 保護調配物達成。 因此,本發明係關於較佳呈水性微乳液形式之液態水性 143575.doc 201018400 植物保護調配物,其包含 a) 至少一種2(TC下之水溶解度小於5 g/l的有機植物保護 劑; b) 至少一種20°C下之水溶解度大於100 gM、尤佳至少200 g/Ι或至少3 00 g/Ι的有機溶劑(溶劑b); c) 至少一種20°C下之水溶解度介於2 g/1至1〇〇 g/l之間、 尤佳介於3 g/Ι至90 g/Ι之間或介於4 g/Ι至80 g/Ι之間的 有機溶劑(溶劑c); d) 至少一種20°C下之水溶解度小於2 g/l、尤佳至多1 g/l 或至多0.5 g/l的有機溶劑(溶劑d); e) 至少一種非離子型表面活性劑; f) 至少一種陰離子型表面活性劑;及 g) 水。 因此’本發明進一步係關於本發明植物保護調配物用於 處理植物或種子之用途及相應方法。本發明進一步係關於 經該植物保護調配物處理之種子。 【實施方式】 特定言之,本發明調配物提供用於處理植物及種子(較 佳為種子)之有機水不溶性植物保護劑之穩定水性調配 物’該有機水不溶性植物保護劑較佳為殺真菌劑且視情況 與其他有機植物保護劑組合。 通常’本發明調配物係微乳液,即各組份形成包含至少 個有機相及一個水相之多相系統,平均相界距離(通常 為刀散相之平均粒經或微滴尺寸=藉由光散射測定之平 143575.doc 201018400 均直徑))通常不大於500 nm ^與懸浮濃縮物相反,活性物 負不以固體形式而是以溶解形式存於本發明調配物中。因 此’本發明調配物亦可稱為ME調配物。本發明調配物係 .穩定液態調配物,其在視覺上係透明的且在儲存時不易產 • 生固體。而且,其在低至_1〇〇c以下之溫度下仍保持液態 而不失去其有利特性。其凍結溫度通常在_1(rc以下。 通常’本發明調配物之動力學黏度不超過0.5 pas(在 ❼ 2〇C下),且通常在20°C下介於1 mPa.s至500 mPa,s範圍 内’且尤佳介於2mPa.s至200 mPa.s範圍内。 而且’本發明調配物可容易地用水稀釋。例如,本發明 調配物可在施用之前簡單地用水稀釋,例如每份調配物用 0.1至100份水’尤佳每份調配物用0 5至50份水,且無粗糙 微粒物質形成。通常,本發明調配物以未經稀釋形式或相 對少量水之稀釋物形式使用,通常每份調配物不多於5份 水且較佳不多於2份水。在本文中,用於稀釋之水的品質 φ 不甚重要,意味著可使用例如自來水或泉水。 本文ic及之平均顆粒直徑代表可藉由光散射測定之顆粒 直徑的Z平均值。熟習此項技術者所熟習之相關方法闡述 於以下文獻中:例如,H. Wiese(D. Distler編寫),WSssrige Polymerdispersionen [Aqueous polymer dispersions], Wiley-VCH 1999,第4.2.1章,第40頁及以後,及其中所引用之 文獻;H. Auweter,D. Horn,J. Colloid Interf. Sci. 105 (1985),第 399頁;D. Lilge,D. Horn,Colloid Polym. Sci· 269 (1991) ’ 第 704 頁;及 H. Wiese,D. Horn, J. Chem. 143575.doc 201018400
Phys· 94 (1991),第6429頁。由於用水稀釋後粒徑較小, 因此與傳統調配物相比生物利用度且因此生物活性通常提 南。 通常’本發明調配物係水包油乳液,其中溶解有部分溶 劑之水(=水相)構成連續相,而另一部分溶劑及一或多種 植物保護劑(=油相)存在於分散相中。然而,在一些情形 下,其為油包水乳液’其中溶解有部分溶劑之水(=水相) 構成非連續相,而另一部分溶劑及一或多種植物保護劑(= 油相)存在於連續相中。本發明調配物亦可以雙連續相存 在’即水相與油相形成互相貫穿的相。 下文所用之術語「烷基」、「烯基」、「伸烷基」、 「芳基」係各情形下某些有機基團之統稱。在本文中,前 綴Cn-Cm表示各情形下各有機基團之碳原子總數。對於溶 劑,則綴cn-cm表示各情形下各有機溶劑之碳原子總數, N-甲基取代之雜環溶劑(例如N_甲基内醯胺及甲基·或 N,N-二甲基脲)除外,其中前綴Cn_Cm表示各情形下雜環之 碳原子總數;磷酸三烷基酯亦除外,其中前綴Cn Cm表示 各烷基基團之碳原子數。 術語「烷基」係指具有前綴中所述碳原子數之飽和直 鏈、具支鏈或環狀烴基團。因此,(Ci_C7)_烷基係指具有^ 個至7個碳原子之飽和直鏈、具支鏈或環狀烴基團例 如,甲基、乙基、丙基、卜甲基乙基、丁基叫甲基丙 基、2-曱基丙基、U_二甲基乙基、戊基、!甲基丁基、 2-甲基丁基'3-甲基丁基、以二甲基丙基、卜乙基两 143575.doc 201018400 基、環戊基、己基、1,1-二甲基丙基、12_二甲基丙基、卜 甲基戊基、2-甲基戊基、3 -甲基戊基、4-甲基戊基、1,1-二甲基丁基、1,2-二甲基丁基、ι,3-二甲基丁基、2,2-二甲 基丁基、2,3-二曱基丁基、3,3-二甲基丁基、卜乙基丁基、 2-乙基丁基、l,i,2-三曱基丙基、三曱基丙基、卜乙 基-1-甲基丙基、1-乙基-2-曱基丙基、環己基、甲基環戊 基、庚基、1-甲基己基、2-甲基己基、3 -甲基己基、4-甲 基己基、1,1,3-三甲基丁基、i,2_二甲基戊基、13二甲基 戊基、2,2-二曱基戊基、2,3·二甲基戊基、3,3_二曱基戊 基、3,4-二曱基戊基、1-乙基戊基、2_乙基戊基、^2三 曱基丁基、1,2,2-二曱基丁基、卜乙基j曱基丁基、卜乙 基-2-曱基丁基、甲基環己基、152_二甲基環戊基、u-二 甲基環戊基及乙基環戊基。 術語「Cz-C4·伸烷基」係指具有2個、3個或4個碳原子之 飽和二價直鏈或具支鏈烴基團,例如,乙烷_丨,2_二基、丙 φ 烷_1,3·二基、丙烷胃1,2-二基、2-甲基丙烷-U·二基、丁 烷-1,4-二基、丁烷-1,3-二基卜曱基丙烷^,%二基)、丁 烷-1,2-二基及丁烷-2,3-二基。 • 術語「芳基」係指芳香族基團,其包括具有丨個或2個選 自Ο及N之雜原子的雜芳香族基團,例如,苯基、萘基、 蒽基、吡啶基、吡咯基、吡嗪基、嘧啶基、嘌呤基、吲哚 基、喹啉基、異喹啉基、咪唑基、吡唑基、吲唑基、呋喃 基、苯并MS、異料料&、嗎琳基、料基、苯并 噁°坐基、異噁°坐基及苯并異噁唑基。 143575.doc •11· 201018400 本發明調配物包含至少一種20°C下之水溶解度大於1 〇〇 g/Ι、尤佳至少200 g/Ι或至少300 g/Ι之溶劑b)。溶劑b)可選 自許多種極性有機溶劑。其較佳選自羥基化之 烴羧酸酯、脂族(C2_C8)-二醇及三醇(尤其脂族(c5_c8)-二 醇及三醇)、(Cs-C8)-烷烴羧酸烷氧基烷基酯、二甲基亞砜 (DMSO)、四氫糠醇、(c3-C4)-碳酸伸燒基醋、n,N,-二甲 基-(C3-C5)-伸燒基脲、(C3-C5)·内酯、N-甲基_(C3-C5)-内醯 胺及磷酸三-(C丨-C3)烷基酯。 在本發明範圍内’術語「羥基化之(C4-C8)-烷烴羧酸 酷」係指經烧醇醋化之院烴緩酸之酯,其中源自酸之烧基 基團或源自醇之烷基基團經至少一個羥基取代,且其中碳 原子之總數為4至8。羥基化之烷烴羧酸之實例係5 _經基戊 酸、4-經基戊酸、2-經基戊酸、4-經基丁酸、3-經基丁 酸、2-羥基丁酸、3_羥基丙酸、乳酸及羥基乙酸。經基化 之烧醇之實例係戊烷_1,5_二醇、戊烷-丨}二醇、戊院·2,4_ 二醇、環戊烷-1,2-二醇、丁烷-1,4-二醇、丁燒 _2,3,_二 醇、丙烷-1,2-二醇、2-(羥基曱基)丁醇、2-(羥基乙基)丙 醇、2-(經基曱基)丙醇及乙烧-1,2 -二醇。經基化之(c5_c8)_ 院烴羧酸酯之實例係4-羥基丁酸正丁基酯、3_羥基丁酸異 丁基酯、4-羥基丁酸正丙基酯、4-羥基丁酸異丙基酯、3_ 經基丁酸異丙基酯、4-羥基丁酸曱基酯、4-羥基丁酸乙基 醋、乳酸2-乙基丙基酯、乳酸2-甲基丙基酯、乳酸正丙基 醋、乳酸異丙基酯、乳酸正丁基酯、乳酸異丁基酯、乳酸 乙基酯、乳酸曱基酯、乳酸環戊基酯、羥基乙酸正己基 143575.doc -12· 201018400 酯、羥基乙酸環己基酯、羥基乙酸3_曱基環戊基酯、羥基 乙酸正戊基酯、羥基乙酸2-甲基戊基酯、羥基乙酸正丁基 酯、羥基乙酸第三丁基酯、羥基乙酸正丙基酯、羥基乙酸 異丙基酯、乙酸5-羥基戊基酯、丙酸3_羥基環戊基酯、乙 酸3-羥基丁基酯、乙酸3·羥基丙基酯、丙酸3_羥基戊基 酯、丙酸3-羥基環戊基酯、丙酸2_羥基甲基丁基酯、丙酸 3-羥基丙基酯、丙酸2-羥基乙基酯、丁酸2_羥基曱基丙基 φ 酯、丁酸3-羥基丙基酯、丁酸2-羥基乙基酯、戊酸3·羥基 丙基酯及戊酸2-羥基乙基酯。 在本發明範圍内,脂族醇及三醇應理解為意 指具有2個至8個且尤佳5個至8個碳原子之附接2個或3個羥 基的脂族直鏈或具支鏈烴,例如丨,5_戊烷二酵、2,4-戊烷 二醇、2-曱基-2,4-戊烷二醇(己二醇)、U6_己烷二醇、2,5· 己烷二醇、3_曱基-2,4·己烷二醇、1,7-庚烷二醇、2,6-庚烷 二醇、M-辛燒二醇、2,7_辛烷二醇、I%環己烷二醇、 • 1,2_環己烧二醇、丨,4-環己烷二醇、I,2-環庚烷二醇、 1,2,3-戊烷三酵、2,3,4_戊烷三醇、丨,2,3_己烷三醇、丨,2,5· 己烷三醇、1,2,3-庚烷三醇、i,6,7_庚烷三醇、2,3,6_庚烷 二醇、1,2,3-辛烷三醇、2,3,4_辛烷三醇丨,2,8_辛烷三醇、 2,3,7-辛烷二醇、環己烷三醇、丨,3,5_環己烷三醇、 1,2,4-環己院三醇、環庚烷三醇及〗,2,6•環庚烷三 醇。 在本文中’(Cs-C8)-烷烴羧酸烷氧基烷基酯應理解為意 指烷烴羧酸與烷氧基烷醇之酯,其中碳原子總數為5至8。 143575.doc -13· 201018400 實例係甲酸異丙氧基曱基酯、乙二醇乙基醚甲酸酯、乙二 醇丁基醚曱酸酯、乙二醇2-曱基丁基醚甲酸酯、乙二醇戊 基醚f酸酯、甲酸異丙氧基甲基酯、甲酸異丙氧基乙基 酯、甲酸異丙氧基第三丁基酯、乙酸乙氧基甲基酯、乙酸 異丙氧基甲基酯、乙二醇甲基醚乙酸酯、乙二醇乙基醚乙 酸醋、乙二醇丙基醚乙酸酯、乙二醇丁基醚乙酸酯、乙二 醇第三丁基醚乙酸酯、丙二醇甲基醚乙酸酯、丙二醇乙基 醚乙酸醋、丙二醇丙基醚乙酸酯、丙二醇異丙基醚乙酸 S旨、乙酸甲氧基丙基酯、乙酸乙氧基丙基酯、乙酸丙氧基 參 丙基醋、乙酸異丙氧基丙基酯、乙二醇曱基醚丁酸酯、乙 二醇乙基趟丁酸酯、丙二醇甲基醚丁酸酯、丙二醇甲基醚 2-甲基丙酸酯、丁酸異丙氧基甲基酯、第三丁酸丙氧基甲 基酯、丁酸甲氧基丙基酯、2_甲基丙酸曱氧基丙基酯、乙 二醇甲基醚戊酸酯及乙二醇甲基醚3_甲基丁酸酯。 在本文中,(CyC4)-碳酸伸烷基酯特定言之係指具有總 共3個至4個碳原子之碳酸環狀二酯,例如碳酸乙二酯、碳 酸1,3-丙二酯及碳酸丨,2_丙二酯。 φ 1-C3)烷基酯應理解為意指磷酸與三個(CrCJ烷
基酯、磷酸乙基2- 甲基丙基曱基酯及磷酸二 二乙基正丙基 磷酸三 醇之三酯, 143575.doc • 14 - 201018400 Ν,Ν·—甲基-(c^-c:4)伸烷基脲應理解為意指環中具有3個 或4個碳原子之環狀脲之二_N_甲基化衍生物。N,N,_二曱 基-(C3-cs)伸烷基脲之實例係N,N,_二曱基伸乙基脲(ι,3二 曱基味唾琳-2-酮)。 (C3_C5)-内醋應理解為意指環中具有3個、4個或5個碳原 子之羥基羧酸環狀酯。(C3_C5)_内酯之實例係丁内酯。 Ν-甲基-(CVC5)-内醯胺應理解為意指環中具有3個、*個 參或5個碳原子之内醢胺的N_甲基化衍生物。N_甲基气q· C5)-内醯胺之實例係N-曱基吡咯啶酮及N_f基六氫吡啶 _。 根據一較佳實施例,本發明調配物包含至少一種溶劑 b),其選自二甲基亞砜、羥基化之(C4_C8)_烷烴羧酸酯、 脂族(c^c:8)-二醇及三醇(尤其脂族(C5_C8)_二醇及三醇)、 (C5-Cs)-院煙緩酸烧氧基烧基醋、四氫糠醇、n_曱基_(〇4_ CS)-内醯胺及(C4_C5)-内酯,且其尤佳選自丁内酯、二甲 φ 基亞砜、乙酸甲氧基丙基酯、2-曱基-2,4-戊烷二醇、己二 醇(1,6-己烷二酵)、四氫糠醇及乳酸正丙基酯。 在一尤佳實施例中,本發明調配物包含二曱基亞砜作為 該至少一種溶劑b)。 根據另一尤佳實施例,本發明調配物包含二曱基亞硬作 為一種溶劑b)且包含至少一種第二溶劑b),該至少一種第 二溶劑b)並非二甲基亞砜且較佳選自羥基化之(C5_c8)烷烴 叛酸酯、脂族(Cs-C8)-二醇及三醇、(C5_c;8)_烷烴羧酸烷氧 基烧基酯、((VC4)碳酸伸烧基酯、γ_ 丁内酯、N_甲基 143575.doc •15- 201018400 c:5)-内醯胺及磷酸三(Cl_C3)烷基酯,尤佳選自丫_丁内酯、 乙酸甲氧基丙基S旨、2-甲基-2,4-戍垸二醇、己二醇、四复 糠醇及乳酸正丙基酯。 根據一同樣尤佳之實施例,本發明調配物包含佔調配物 總重量小於(Μ重量%之二甲基亞礙。根據本發明之該實施 例,該至少一種第二溶劑b)較佳選自羥基化之(C5_Cs)烷烴 羧酸酯、脂族(eves)-二醇及三醇、烷烴羧酸烷氧 基烷基酯、四氫糠醇、(C4_C5)_内酯及N_甲基兴C4_c5)_内 醯胺,尤佳選自γ-丁内醋、乙酸甲氧基丙基醋、2甲基-❿ 2,4-戊烷二醇、己二醇〇,6_己烷二醇)、四氫糠醇及乳酸正 丙基醋。 通常,存在於本發明調配物中之溶劑…的總量端視有機 植物保護劑a)、表面活性劑e)Af)及溶劑e)及d)的量及其特 I·生而疋。溶劑b)與植物保護劑a)之總量的重量比通常介於 0.05:1至30:1範圍内,較佳介於〇 1:1至1〇:1範圍内且尤佳 "於0.15:1至5:1範圍内。溶劑b)的量通常為未經稀釋調配 物總重量之1重量%至6〇重量%,較佳1〇重量%至4〇重量% 〇 且尤佳15重量%至35重量%。在包含DMS◦作為唯—溶齊⑻ 之調配物情形下’ DMs〇的量較佳佔調配物總重量之不大 於5重量%,例如!重量%至5重量%。在含有dms〇與至少 種其他,谷劑b)之組合之調配物情形下,DMS〇與該其他 浴劑bX重量比通常介於1:2()至1:1範圍内尤佳介於 =1.2範圍内。在該等調配物中’ 的量較佳佔調配物 總重量之不大於5重量%,例如0.5重量%至5重量%。 143575.doc • 16 · 201018400
本發明調配物包含至少一種20°C下之水溶解度介於2 gM 至100 g/1之間、尤佳介於3 g/1至90 g/1之間或介於4 g/1至
80 g/Ι之間的溶劑c)。溶劑c)可選自許多種中等極性之有機 溶劑。其較佳選自(C5-C9)-烷烴羧酸烷基酯、(C9-C12)-烷烴 羧酸烷氧基烷基酯、(C5_C9)_二羧酸二烷基酯、(C5-C9)-酮、((VC9)-芳基烷基醇、(cvc9)-芳氧基烷基醇、(c5-C9)-環烧基醇、(C5-C9)-烷烴二醇烷氧化物、(C5_c9)_烷烴 二醇院氧化物及(C5-C6)-碳酸伸院基g旨。 在本文中’特定言之,(C5_C9)-烷烴羧酸烷基酯應理解 為意指碳原子總數為5至9且尤其為5、6、7或8之經烷醇酯 化之烷烴羧酸。實例係乙酸異丙基酯、乙酸正丙基酯、乙 酸異丁基酯、乙酸第三丁基酯、乙酸正戊基酯、乙酸環戊 基酯、乙酸正己基酯、乙酸3_曱基環戊基酯、乙酸環己基 0曰、乙酸正庚基酯、乙酸3_甲基環己基酯、丙酸正丙基 酯、丙酸異丙基酯、丙酸正丁基酯、丙酸第三丁基酯、丙 酸正戊基S曰、異丙酸正丙基酯、丙酸環丙基酯、異丙酸環 丙基酿、異丙酸異丙基酯、異丙酸正丁基醋、異丙酸第三 丁基S曰、異丙酸正戊基酯、丙酸正己基酯、丙酸環己基 酯 丁鲛乙基自曰、丁酸正丙基酯、丁酸異丙基酯、丁酸正 丁基酯、丁酸第三丁基酯、第三丁酸乙基酯、第三丁酸正 丙基S曰、第二丁酸異丙基酯、第三丁酸正丁基酯、第三丁 酸第三丁基醋、丁酸不士、I沾 馱正戊基a曰、戊酸甲基酯、戊酸乙基 曰戍酸丙基S曰、戊酸異丙基酯、戊酸正丁基酯、己酸甲 基醋、己酸乙基醋、己酸異丙基酿、庚酸甲基醋、庚酸乙 143575.doc •17- 201018400 基醋及辛酸甲基醋。 在本文中,(c9_Cl2)燒㈣酸烧氧基烧基g旨應理解為意 指烧烴缓酸與燒氧基燒醇之醋,其中石炭原子總數為9至 12。實例係乙酸異丙氧基丁基酯、乙二醇丙基醚丁酸醋、 乙二醇戊基醚丙酸酯、乙二酵2_曱基丁基醚甲酸酯、丙二 醇乙基縫戊酸醋、丙二醇丁基鍵2_甲基丙酸醋、丁酸異丙 氧基丙基酯、第三丁酸丙氧基戊基酿、丁酸乙氧基丙基 酯、2-乙基丙酸乙氧基丙基酯、乙二醇乙基醚己酸酯、乙 二醇丙基醚3-甲基戊酸酯、庚酸乙氧基甲基酯、己酸乙氧 基丁基酯及3-乙基丁酸曱氧基丙基酯。 在本文中,(Cs-C9)-二羧酸二烷基酯應理解為意指烷烴 二羧酸與兩個彼此獨立地加以選擇之烷酵之二酯,其中碳 原子總數為5至9且尤其為5、6、7或8。實例係草酸乙基酯 甲基醋、草酸二乙基醋、草酸乙基酯丙基醋、草酸乙基酯 異丙基酯、草酸二丙基酯、草酸丙基酯異丙基酯、草酸乙 基酯丁基酯、草酸曱基酯戊基酯、草酸丙基酯丁基酯、丙 二酸二甲基酯、丙二酸甲基酯乙基酯、丙二酸二乙基酯、 丙二酸丙基酯乙基酯、丙二酸異丙基酯乙基酯、丙二酸甲 基酯丙基酯、丙二酸甲基酯異丙基酯、丙二酸二丙基酯、 琥珀酸二甲基酯、琥珀酸乙基酯甲基酯、琥珀酸二乙基 酯、琥珀酸甲基酯丙基酯、琥珀酸甲基酯異丙基酯、琥珀 酸乙基酯丙基酯、戊二酸二甲基酯、戊二酸乙基酯甲基 酯、戊二酸二乙基酯、己二酸二甲基酯、己二酸乙基酯甲 基酯及庚二酸二甲基酯。 143575.doc •18- 201018400 在本發明範圍内,術語「(c^c:9)-酮」包含具有5個至9 個碳原子之視情況烷氧基化之脂族、環脂族及芳脂族酮; 該等包括例如2-戊酮、3-戊酮、2-己酮、3-己酮、2-庚 酮、3_庚酮、4·庚酮、2-辛酮、3-辛酮、4-辛酮、4-甲基-2-戊酮、5-甲基-2-己酮、環戊酮、環己酮、環庚酮、環辛 嗣、環己基竣基甲烧、苯乙酮及甲氧基苯乙酮。 (Cs-C9)-芳基烷基醇(=芳基烷醇)應理解為意指經芳基基 $ 團取代之烷醇,該(Cs-C9)-芳基烷基醇包含5個至9個碳原 子。實例係苯曱醇、2-苯基乙醇、卜苯基乙醇、苯基丙 醇、吡啶-1-基甲醇、吡啶·3-基甲醇、卜吡啶_3_基乙醇、 吡啶基丁醇、嘧咬-1-基曱醇、嘧啶_丨_基乙醇、2_嘧咬_3_ 基丙醇、呋喃-2-基曱醇、2-呋喃_2_基乙醇、3-呋喃-3-基 丙醇及4-呋喃-2-基丁醇。 (Cs-C:9)-芳氧基烷基醇(=芳氧基烷醇)應理解為意指經芳 氧基基團取代之烧醇,該(C5_C9)·芳氧基烷基醇包含5個至 參 9個碳原子。實例係苯氧基甲醇、苯氧基乙醇及苯氧基異 丙醇。 在本文中’(Cs-C9)-環烷基醇係指具有5個至9個碳原子 之環狀烧醇,例如,環戊醇、環己醇、環庚醇及環辛醇。 在本文中’(CVC9)-烷烴二醇烷酸酯應理解為意指經兩 個烷酸酯化之烷烴二酵’其中該烴二醇烷氧化 物包含5個至9個碳原子。實例係甘油二乙酸酯(diacetin)、 二酵二乙酸酯、二醇二丙酸酯、甘油二丙酸酯及丙二醇二 乙酸酯。 143575.doc -19· 201018400 在本文中,(Cs-C9)-烷烴三醇烷酸酯應理解為意指經三 個烧酸醋化之院烴三醇,其中該OVCO·炫烴三醇烧氧化 物包含5個至9個碳原子。實例係甘油三乙酸醋。 在本文中’(CVC6)-碳酸伸烷基酯特定言之係指碳酸之 具有5個至6個碳原子之環狀二酯,例如,碳酸1,2-丁二酯 及碳酸2,3-丁二酯。 根據一較佳實施例,本發明調配物包含至少一種溶劑 O’其選自(cvc+嗣、(C5_C9)_芳基烷基醇、(C5_C9)芳氧 基烷基醇、(c5-c9)_烷烴三醇烷酸酯及(C5_C6)_碳酸伸烷基 S曰且尤佳選自苯乙嗣、苯甲醇、環己嗣、2_庚嗣、甘油 三乙酸酯、碳酸丁二酯及2-苯氧基乙醇。 存在於本發明調配物中之溶劑〇的總量通常端視有機植 物保護劑a)、表面活性劑似〇、及溶劑b)及d)的量及其特 性而定。溶劑c)與植物保護劑a)之總量的重量比通常介於 至3〇,1|&圍内,較佳介於0·1:1至20:1範圍内且尤佳 介於〇.5:!至1():1範圍内。溶劑e)的量通常為未經稀釋調配 物總重量之1重量%至6()重量%,較佳ig重量%至⑽重量% 且尤佳15重量%至35重量%。 本發明調配物包含至少一種2代下之水溶解度小於2 g/】、較佳至多1 、去 夕0.5 g/】的溶劑d)。溶劑d)可 選自多種非極性溶劑,例如 例如知族或芳香族烴、植物油、 脂肪酸及其衍生物。溶 坪J )校住選自沸點介於100eC至 3 I 0 °c間之脂族、芳香族 ^广、 及環月曰族烴、(Cs-C20)-烷基酚、 挖醇、心.w幾酸炫基醋、(C9_y 143575.doc -20- 201018400 烧經缓酸烧基醋、(C12-C28)-環烧烴缓酸烧基醋、(C12-C28)-環烷烴二羧酸二烧基酯、(C1G-C15)-二羧酸二烧基酯、 (C25_C35)-烧烴三醇烧酸酯、N-(C6-C18)-烷基-(c3-c5)-内醯 胺、(Cs-C26)-脂肪酸,尤佳(c1(rc2c)-脂肪酸、其二烷基醯 胺(例如其二-Ci-CU-烧基醯胺,例如二甲基醢胺)、及其烧 基酯(例如其Ci-C4-烷基酯,例如曱基酯或乙基酯)。 在本文中,沸點介於100°c至310〇C間、尤佳介於l2(rc 至280°c間(常壓)之脂族烴特定言之係指直鏈及具支鏈烷烴 或烯烴’其具有7個至約18個碳原子且在常壓下具有上述 範圍内之沸點,尤佳亦為該等脂族烴之混合物。該等混合 物可以例如商標名Exxs〇1購得,該等產品主要包含脫芳香 族成份已脫去之石油’例如,Exxs〇l D3〇、Exxs〇1 D4〇、
Exxsol D80、Exxsol m〇〇、Exxs〇1 D12〇 及 Εχχ3〇ι D220/230。 在本發明範圍内,沸點介於1〇〇£>c至31〇£>(:間、尤佳介於
120 C至280 C間(常壓)之芳香族烴應理解為意指視情況附 接-或多個脂族或芳脂族取代基(尤㈣基或芳基烧基基 ,)且在常壓下具有上述^圍内之I點的單環狀及多環狀 芳香、化口物。其較佳理解為意指(特定言之)礦物油產品 在上料點範圍内蒸財以齡形式獲得之芳香族烴之混 合物’例如以下列商標名習知之市售產品:3〇卜奶。@,特 定言之 S〇lvesso@ 100、S— 150、Solvesso@ 2〇〇、 W彻^ 15〇 ND、S0lvess0@ 2〇〇 ND ;芳香族 (Ar〇matlc) ’特定言之芳香族⑧⑽及芳香族⑧2〇〇 ;水溶 143575.doc -21 - 201018400 膠(Hydrosol)®,特定言之水溶膠® A 200及水溶膠® a 230/270 ** Caromax®,特定言之 Caromax® 20及 Caromax® 28 ; Aromat K 150、Aromat K 200 ; Shellsol®,特定言之 Shellsol® A 100 及 Shellsol® A 150 ;及 Fin FAS-TX,特定 言之Fin FAS-TS 150及Fin FAS-TX 200。尤佳者係混合物 Solvesso® 150 ND 及 Solvesso® 200 ND (ExxonMobil Chemical),其中潛在致癌物質萘已脫去。因此, Solvesso® 150 ND主要包含具有10個或11個碳之芳香族 烴’其沸點介於175°C至209°C之間且主要為烷基苯,而 Solvesso® 200 ND主要包含具有1〇個至14個碳之芳香族 烴,其沸點介於235°C至305°C之間且主要為烷基萘。本文 所述芳香族烴之又一實例係可以商標名Hisol SAS-296購得 之產品’其為1-苯基-1-二甲苯基乙烷與1_苯基_丨_乙基苯基 乙烧之混合物。 在本發明範圍内’沸點介於100°C至3 1 〇°c間、尤其介於 120°C至280°C間(常壓)之環脂族烴應理解為意指包含非芳 香族碳環之飽和及非飽和烴及該等烴之混合物。實例係擰 檬烯。 術語(Cs-Cm)-烷基酚係指在環上經至少—個烷基基團取 代之酚,該(Cs-C^o)-烷基酚具有8個至2〇個碳原子。實例 係乙基酚、2-甲基-4-乙基酚、二庚基酚及十二烷基酚。 在本文中,(Cs-Cso)-烷醇應理解為意指具有8個至2〇個 碳原子之烷醇,尤其具有8個至14個碳原子之烷醇(=(c8. Cm)-烷醇)。實例係辛醇、癸醇、十二烷醇、十三烷醇、 143575.doc •22- 201018400 壬醇、異壬醇、2-丙基庚酵及乙基己酵。 在本文中’特定言之’(C1G_c2Q)-烷烴羧酸烷基酯應理解 為意指碳原子總數為1〇至2〇之經烷醇酯化之(Cl_C9)_烷烴 羧酸。貫例係乙酸乙基己基酯、乙酸正壬基酯、乙酸異莰 基醋、異丙酸丙基庚基酯、丁酸正癸基酯、己酸第三丁基 醋、辛酸正戊基-4-乙基酯及壬酸乙基酯。 在本文中’特定言之,羥基烷烴羧酸烷基酯應 理解為意碳原子總數為9至2 〇之經烧醇g旨化之經基化之 烷烴羧酸,尤其為乳酸(乳酸酯)。通常,烷基基團具有3個 至1 〇個C原子。實例係3-羥基癸酸第三丁基酯、4_羥基辛 酸正丙基酯、4-羥基辛酸異丙基己基酯、3·丙基羥基己 酸乙基酯、4-羥基丁酸正戊基酯、3_羥基丁酸乙基己基 醋、乳酸2-乙基戊基酯、乳酸癸基酯、乳酸乙基己基酯、 羥基乙酸正庚基酯、羥基乙酸環己基乙基酯及羥基乙酸3_ 異丙基環戊基醋。 在本文中’(Cu-C28)-環烷烴羧酸烷基酯或 烧烴二羧酸二烷基酯應理解為意指分別經一個或兩個叛基 取代且分別經一個或兩個烧醇酯化之碳原子總數為丨2至Μ 之環烷烴。實例係環戊烷羧酸己基酯、環己烷缓酸戊基 酉曰、%己炫叛酸3-異丙基己基醋、1,2 -環戊烧二叛酸二丁 基酯、1,3-環戊烷二羧酸乙基酯丁基酯、i,2_環己烧二叛 酸二癸基酯、1,4-環己烷二羧酸曱基酯辛基酯及環己烧二 羧酸二異壬基酯。 在本文中’(C^-C!5)-二羧酸二烷基酯應理解為意指碳原 143575.doc •23- 201018400 子總數為10至15之烧煙二譏^酸與兩個烧醇之二醋。通常, 烧基基團具有2個至8個C原子。實例係草酸丁基醋己基 酯、草酸二戊基酯、丙二酸二異丁基酯、丙二酸二己基 Θ旨、丙一酸乙基醋戍基S旨、玻拍酸二丙基醋、破拍酸二異 丙基酯、琥珀酸二異丁基s旨、琥珀酸二戊基酯、戊二酸二 異丙基酯、戊二酸二異丁基酯、戊二酸乙基酯戊基酯、戊 二酸二環戊基酯、己二酸二異丁基酯、己二酸乙基酯丙基 酯、庚二酸二異丁基酯及庚二酸二乙基酯。 在本文中,(C25_C35)-烷盤三醇烷酸酯應理解為意指經三 個烧酸醋化之烧烴三醇,其中(C25_C35)_烷烴三醇烷酸酯包 含25個至35個碳原子。實例係Myritol® 312 (Cognis),其 為甘油三酸酯與(C8_C1G)-脂肪酸殘基之混合物。 在本文中,N-CCVC^)-烷基内醯胺應理解為意 指環中具有3個、4個或5翻碳原子之N-烷基化之内醯胺衍 生物,其中N-烷基基團包含6個至18個碳原子。實例係N-辛基°比嘻咬酮。 在本文中’(Cs-C26)-脂助酸應理解為意指具有8個至26 個碳原子之脂肪酸。實例愈飽和脂肪酸辛酸、癸酸、月桂 酸、肉豆慈酸、椋櫚酸、汁七烧酸、硬脂酸、花生酸、二 十二烷酸、二十四烧酸及二十六烷酸;及單不飽和脂肪酸 十一碳烯酸、棕櫊油酸、由酸、反油酸、異油睃、二十碳 烯酸(icosenoic acid)、鯨嘴烯酸、芥酸及神經酸;及多不 飽和脂肪酸亞油酸α-亞麻酸、γ_亞麻酸、花生四稀酸、二 十碳五烯酸、二十二碳五_烯酸及二十二碳六烯酸。(Cs- 143575.doc •24- 201018400 。26)-月旨肪酸之二炫*基酿胺的實例係上述脂肪酸之二_Ci-C4-烷基醯胺,例如二甲基醯胺、二乙基醯胺、二丙基醯胺、 二異丙基醯胺、二丁基醯胺、二異丁基醯胺、甲基乙基醯 胺、甲基丙基醯胺、甲基異丁基醯胺、甲基第三丁基醯 胺、乙基丙基醯胺、乙基異丙基醢胺、乙基丁基醯胺、乙 基異丁基醯胺、丙基異丙基醯胺、丙基丁基醢胺及丙基異 丁基酿胺’尤佳為·一甲基酿胺。(C8-C26)-脂肪酸之炫基画旨 的實例係上述脂肪酸之烷基酯,例如曱基酯、乙基 ^ 酯、丙基酯、異丙基酯、丁基酯、異丁基酯、第三丁基 酯、1-甲基丙基酯、戊基酯、1-甲基丁基酯、2_甲基丁基 酯、3-曱基丁基酯、己基酯、丨_甲基戊基酯、2_甲基戊基 醋、1-乙基丁基酯及1,2-二曱基丁基酯、庚基酯、丨_甲基 己基酯、2_甲基己基酯、3-甲基己基酯、4-曱基己基酯、 5-甲基己基酯、1-乙基戊基酯、2-乙基戊基酯、3-乙基戊 基醋、4·乙基戊基酯、ι,2-二甲基戊基酯、i,3_二曱基戊基 φ 輯、I4-二曱基戊基酯、2,3-二曱基戊基酯及乙基_2_甲基 丁基酯’尤佳為甲基酯及乙基酯。 根據一較佳實施例,本發明調配物包含至少一種溶劑 d) ’其選自由(Cg-C:26)-脂肪酸、其二烷基醯胺(例如 一甲基醯胺)、(Ci〇-Ci5)-二羧酸二烷基酯、(C9-C20)-羥基 烷烴羧酸烷基酯組成之群,尤佳為具有總共9個至2〇個^原 子之乳酸酯及在常壓下沸點介於1〇(rc至3 1〇〇c間之芳香族 烴。根據一尤佳實施例,本發明調配物包含至少—種溶劑 )/、選自由下列組成之群.Cl2_C2〇脂肪酸,例如市隹產 143575.doc •25· 201018400 品Edenor® ΤΙ 05 (Cognis),按照製造商說明其為具有高油 酸含量之脂肪酸混合物;Cu-Cu脂肪酸之二甲基醯胺,例 如市售產品Agnique® KE 3658 (Cognis),其為脂肪酸二甲 基醯胺之混合物;(Cs-C!4)-燒醇,例如十二烧醇;在常壓 下/弗點介於120 C至280 C間之芳香族燈,例如s〇ivess〇® 150 ND及Solvesso® 200 ND及類似產品;具有總共9個至 13個C原子之乳酸C6-C10-烧基醋’例如1乳酸2_乙基己夷 酯;及具有總共10個至15個C原子之二羧酸二異丁基醋,
例如琥珀酸、戊二酸及己二酸之二異·7~基酯之工業混合 物0 存在於本發明調配物中之溶劑d)的總量通常端視有機植 物保護劑a)、表面活性劑6)及〇、及溶劑b)&c)的量及其特 性而定。溶劑d)與植物保護劑a)之總量的重量比通常介於 〇·〇5:1至30:1範圍内,較佳介於〇 1:1至2〇:1範圍内且尤佳 介於0.5:1至15:1範圍内。溶劑d)的量料為未經稀釋調配
物總重量之i重量%至60重量%,較佳5重量%至45重量%且 尤佳1 0重量%至35重量%。 在一較佳實施例中,本發明調配物在各情形下僅包含一 種溶劑b)、e)及根據另—較佳實施例,其 含又一種溶劑bhiU)。 卜匕 本發明調配物包含至少一種非離子型表面活性劑e)及 少-種陰離子型表面活性㈣。術語表面活性劑係指表 活性物質,下文中亦稱為乳化劑或清潔劑。表面活性劑 合物之目的係降低連續相與分散相間之表面張力且由此 143575.doc -26- 201018400 疋刀散相之顆粒/微滴。表面活性劑亦有助於溶解該至少 一種有機植物保護劑a)。熟習此項技術者熟習適於調配微 乳液之表面活性劑,例如通過McCutche〇n,清潔劑及乳化 劑公司(Detergents and ⑽郝⑽,Ιη〇編輯,Ridgew〇〇d, 、紐約。表面活性劑可為聚合物或非聚合物表面活性劑。較 佳地’絕大部分(尤其至少9〇%且更尤其全部)存在於微乳 液中之表面活性劑選自由非聚合物表面活性劑(其亦稱為 • 乳化劑)組成之群。通常,«合物表面活性劑(乳化劑)具 有至多2000道爾頓、較佳15〇道爾頓至2〇〇〇道爾頓且尤佳 2〇〇道爾頓至1500道爾頓之平均分子量(平均數)。 非離子型表面活性劑群組特定言之包含: • (CVC4)-環氧烷之均寡聚物或共寡聚物,例如環氧乙 烧、環氧丙垸(=甲基環氧乙统)、1>2•環氧丁烷(=^ 乙基環氧乙烧)及2-甲基環氧丙烧(=二甲基環氧乙 烷)之均募聚物或共寡聚物,尤其環氧乙烷之均寡聚 • 物、環氧丙烷之均寡聚物及環氧乙烷/環氧丙烷共募聚 物; 寡聚(CVC4)-環氧烧(Cs-C:22)-院基μ,尤其直鍵及具支 鏈(Cs-C22)-烷醇之寡聚乙氧基化物及募聚乙氧基化物_ 共-丙氧基化物,較佳脂肪醇之寡聚乙氧基化物及羰基 ο成醇之寡聚乙氧基化物,例如,月桂醇募聚乙氧基 化物、異十二燒醇寡聚乙氧基化物、録壌醇寡聚乙氧 基化物、硬月曰醇券聚乙氧基化物及其醋,例如,乙酸 酯; I43575.doc -27- 201018400 -寡聚-(CVC4)-環氧烷芳基醚及寡聚_(C2_C4)_環氧烷(Ci_ CJ-烷基芳基醚,例如,寡聚_(C2_C4)_環氧圮(CVC22)_ 烷基苯醚,尤其(Ci-C^)-烷基酚之寡聚乙氧基化物,例 如,壬基酚、癸基酚、異癸基酚、十二烷基酚或異十 二烧基紛之券聚乙氧基化物; -寡聚-((VC4)-環氧烷單·、二_或三苯乙烯基苯基醚,尤 其單-、二-及三苯乙烯基酚之寡聚乙氧基化物、及其與 甲醒之縮合物及其醋,例如,乙酸g旨; -(CVC22)-烷基葡糖苷及((VC22)_烷基寡聚葡糖爷; -(CVC22)-烷基葡糖苷之寡聚乙氧基化物及(c6·c^_烷基 寡聚葡糖苷之寡聚乙氧基化物; -脂肪酸之寡聚乙氧基化物及羥基脂肪酸之寡聚乙氧基 化物; -多7C醇與(CrC22)-烷酸之部分酯,尤其甘油之單酯及二 醋及山梨糖醇酐之單酯、二酯及三酯,例如,甘油單 硬脂酸酯、山梨糖醇酐單十二烷酸酯、山梨糖醇酐二 油酸酯及山梨糖醇酐三硬脂酸酯; -多兀醇與(CrC22)-烷酸之邹分酯的寡聚乙氧基化物,尤 其甘油之單酯及二酯的募聚乙氧基化物及山梨糖醇酐 之單酯、二酯及三酯的募聚乙氧基化物,例如,甘油 單硬脂酸酯之寡聚乙氧基化物、山梨糖醇酐單油酸酯 之寡聚乙氧基化物、山梨糖醇酐單硬脂酸酯之募聚乙 氧基化物及山梨糖醇酐三硬脂酸酯之寡聚乙氧基化 物; 143575.doc •28· 201018400 植物油或動物脂肪之寡聚乙氧基化物,例如,玉米油 乙氧基化物、蓖麻油乙氧基化物、妥爾油乙氧基化 物; '炔二醇(acetylene glycol),例如,2,4,7,9-四曱基 _4 7 _ 羥基-5-癸炔; -寡聚氧乙烯/募聚氧丙烯嵌段共寡聚物;及 -脂肪胺或脂肪酸二乙醇醯胺之募聚乙氧基化物。 瘳 術語寡聚-(CVC4)-環氧烷醚或募聚_(C2_C4)_環氧垸係指 衍生自(CrC4)-環氧烷(例如環氧乙烷、環氧丙烷(=丨_曱基 環氧乙烷)、1,2-環氧丁烷(=丨_乙基環氧乙烷)及2_甲基環 氧丙烷(=1,1-二曱基環氧乙烷))之寡聚醚基團。因此,術 語寡聚-(CrC3)-環氧烷醚係指衍生自+環氧烷(例如 環氧乙烷及環氧丙烷)之寡聚醚基團。術語乙氧基化物係 #曰衍生自環氧乙燒之寡聚鍵基團。類似地,術語寡聚環氧 乙烷共-寡聚環氧丙烷係指衍生自環氧乙烷與環氧丙烷之 〇 混合物的聚醚基團。寡聚醚基團中重複單元之數量通常介 於2與120之間,較佳介於4與8〇之間,且尤佳介於5與6〇之 間。 上述非離子型表面活性劑中,以下較佳: -(CrC3)-環氧烧之均寡聚物或共寡聚物, _寡聚_(C2-C4)-環氡烷(C8-C22)-烷基醚, -寡聚-(CVC4)·環氧烷(Ci_Ci6)_烷基苯醚, 寡聚-(C2-C4)-環氧燒單_、二_或三苯乙稀基苯基醚, 券聚(C2 C4)-環氧院單_或二苯乙烯基苯基醚/甲醛縮合 143575.doc •29· 201018400 物, 甘油或山梨糖醇酐與脂肪酸之部分醋,及 ~ 快一醇’及該等之混合物。 在本發明範圍内,尤佳之非離子型表面活性劑包括寡 聚-(Cz-C3)-環氧烷((^-(^+烷基醚、(C2_C3)_環氧烷之均寡 聚物或共募聚物及寡聚-(Q-C3)·環氧烷單_、二_或三苯乙 稀基苯基醚、及該等之混合物。 在本發明之一較佳實施例中’該等調配物之組份e)包含 至少兩種具有不同HLB值之非離子型表面活性劑。根據— 尤佳實施例,該至少兩種非離子型表面活性劑係: e.l)至少一種具有不大於13、尤其為5至13且更尤其為6 至12之HLB值的表面活性劑;及 e.2)至少一種具有大於13、尤其為13 5至18且更尤其為 至17之HLB值的表面活性劑。 在本發明上下文中,術語「HLB值」(「親水親油平衡 值」)係表面活性劑親水性或親油性程度之量度。HLB值 可用於預測分子之表面活性劑特性。根據Davies之方法 (Davies, J.T., Proceedings of the International Congress of
Surface Activity, 1957, 426-438),利用下式來計算該值: HLB = 7 + m * Hh + n * Η1 其中m代表分子之親水性基團的數量,Hh係對應於親水 性基團之特定親水性特徵的值,表分子之親油性基團 的數量’且H1係對應於親油性基團之特定親水性特徵的 值。 i 43575.doc 30- 201018400 具有不大於13之HLB值的非離子型表面活性劑el)可選 自所有上述具有不大於13、尤其5至13或6至12之肌8值的 .非離子型表面活性劑。特定言之,適宜表面活性劑e.”包 • 3养聚_(C2_C4)_環氧烷(C8-C22)-炫基醚、寡聚_(C2_C4)_環 氧烷(C8-C22)-烷基苯醚、山梨糖醇酐單脂肪酸酯及寡聚_ (CVC4)-環氧烷單_、二_或三笨乙烯基苯基醚。該至少一種 非離子型表面活性劑e.1}較佳為募聚_(C2_C4)_環氧烷(c8_ Φ C22)-烷基醚,尤佳為具有介於4至12範圍内之HLB值的寡 聚-(C2_C4)-環氧烧(Cg-C22)-燒基喊。尤佳之非離子型表面 活性劑e.l)選自直鏈或具支鏈(C8_C22)烷醇之寡聚乙氧化 物及养聚乙氧基化物共-丙氧化物。該等較佳表面活性劑 之實例係具支鏈Cl3_醇之乙氧化物’其可以商標名
Lutensol® T03、Lutensol® T05及Lutensol® T07購得。 具有大於13之HLB值的非離子型表面活性劑e 2)可選自 所有上述具有大於13、尤其13.5至18或14至17之HLB值的 φ 非離子型表面活性劑。特定言之,適宜表面活性劑e.2)包 含(CVC3)-環氧烷之均寡聚物及共寡聚物、寡聚_(C2_C3)_ 環氧烷(CVC22)-烷基醚、募聚_(C2_C3)_環氧烷 基苯醚及寡聚-(C^C:3)-環氧烷單_、二或三苯乙烯基苯基 喊。較佳地’該至少一種非離子型表面活性劑e.2)選自 (C:rC3)-環氧烷之均募聚物及共寡聚物及寡聚_(C2_C3)-環 氧烧單-、二-或三苯乙烯基苯基醚,尤佳選自具有介於 13.5至18之間、尤其介於14至17之間之HLB值的(c2-c3)-環 氧烧之均寡聚物及共寡聚物及募聚-(C2-C3)-環氧烷單_、 143575.doc -31- 201018400 二-及三苯乙烯基苯基醚。尤佳之表面活性劑e.2)選自環氧 丙烷/環氧乙烷嵌段共寡聚物及寡聚環氧乙烷三苯乙烯基 笨基醚。該等較佳表面活性劑之實例係三苯乙烯基酚之乙 氧化物,其可以商標名Soprophor®、特定言之Soprophor® S 25及Soprophor® S 40購得;或環氧丙烷/環氧乙烷嵌段共 寡聚物,其可以商標名Pluronic® PE、特定言之Pluronic® PE 6200iLPluronic® 6400購得;或具支鏈(:13-醇之乙氧化 物,其可以商標名[1^6113〇1@丁015購得。 特定言之,陰離子型表面活性劑f)包含以下化合物之鈉 鹽、鉀鹽、辦鹽及錢鹽: -(c6-c22)-烷基磺酸鹽,例如,月桂基磺酸鹽及異十三烷 基磺酸鹽; -(c6-c22)-烷基硫酸鹽,例如,月桂基硫酸鹽、異十三烷 基硫酸鹽、鯨蠟基硫酸鹽及硬脂基硫酸鹽; -芳基磺酸鹽,特定言之(CVCb)-烷基苯磺酸鹽,例如, 異丙苯基磺酸鹽、辛基苯磺酸鹽、壬基苯磺酸鹽及十 二烷基苯磺酸鹽、萘基磺酸鹽、單-及二烷基 萘基磺酸鹽,例如,二丁基萘基磺酸鹽; - 單-及二-(Ci-CM)-烷基二苯基醚(二)磺酸鹽,例如,十 二烷基二苯基醚二磺酸鹽; -脂肪酸及脂肪酸酯之硫酸鹽及磺酸鹽; -寡聚-(c2-c3)-環氧烷(c8-c22)-烷基醚硫酸鹽,特定言之 (c8-c22)-烷醇之乙氧化物的硫酸鹽,例如,月桂醇之乙 氧化物的硫酸鹽; 143575.doc -32- 201018400 -募聚-(Cz-C:3)-環氧烷(Cl_Cl6)-烷基苯醚硫酸鹽,特定言 之(Ci-Ci6)-烧基盼之乙氧基化物的硫酸鹽; -磺基琥珀酸之二-(C4-C18)-烷基酯(=磺基琥珀酸(C4-C18> 二烷基酯),例如,磺基琥珀酸二辛基酯; -萘磺酸、(Ci-C^6)-烷基萘磺酸或苯酚磺酸與甲醛之縮合 物(=(CVCm)-萘磺酸鹽/曱醛縮合物、烧基蔡 磺酸鹽/甲醛縮合物及苯酚磺酸鹽/甲醛縮合物); β -寡聚-(C2_C3)-環氧烷單-、二-及三苯乙烯基苯基醚硫酸 鹽,特定言之單-、二-及三苯乙烯基酚之募聚乙氧化 物; -單-及二-(Cs-C22)-烷基硫酸鹽; -募聚-(Cz-C3)-環氧烷(C8_C22)·烷基醚磷酸鹽; -寡聚-(CVC3)-環氧烷(Cl_Ci6)_烷基苯醚磷酸鹽; -寡聚-(C2-C3)-環氧烷單…二_及三苯乙烯基苯基醚磷酸 鹽; • _寡聚環氧乙烷聚羧酸鹽,特定言之具有3個至8個碳原 子之單乙烯系不飽和單羧酸或二羧酸之均寡聚物及共 ^聚物’其中共寡聚物額外具有募聚環氧乙院側鍵; _脂肪酸,例如,硬脂酸;及 - 寡聚麟酸鹽,例如,丄值βΗ # „ & ,、偏磷酸鹽及三磷酸鹽(或三聚磷 酸鹽)。 在上述陰離子型表面活性劑中 丨王劑T,以下化合物之鈉鹽、鉀 鹽、鈣鹽及銨鹽較佳: -(Ci-C16)-烷基苯磺酸鹽; 143575.doc -33. 201018400 -(CVCm)-烷基萘磺酸鹽; -萘磺酸鹽/曱醛縮合物及(CrCa)-烷基萘磺酸鹽/曱醛縮 合物; -寡聚-(c2-c3)-環氧烷(c8-c22)-烷基醚硫酸鹽; - 寡聚-(c2-c3)-環氧烷(c8-c22)-烷基醚磷酸鹽; -寡聚-(c2-c3)-環氧烷(cvc^)-烷基苯醚硫酸鹽; -寡聚-(C2-C3)-環氧烷(CrCM)-烷基苯醚磷酸鹽; -(C8-C22) -烧基硫酸鹽; - 項基破拍酸(C4-C18)-二烧基醋; -寡聚-(Cz-C3)-環氧烷單-、二-及三苯乙烯基苯基醚硫酸 鹽; -寡聚-(Ca-C3)-環氧烷單-、二-及三苯乙烯基苯基醚磷酸 鹽; -寡聚環氧乙烷I羧酸鹽及 - 聚鱗酸鹽,及該等之混合物。 尤佳之陰離子型表面活性劑〇包含募聚_(C2_C3)_環氧烷 單-、二-及三苯乙烯基笨基醚硫酸鹽,尤其寡聚_(C2_C3)_ 環氧烷單-、二-及三笨乙烯基苯基醚硫酸鈉、寡聚-(c2-C3)-環氧烷單_、二·及三苯乙烯基苯基醚硫酸鉀、寡聚· (CVC3)-環氧烷單、二-及三苯乙烯基苯基醚硫酸鈣及寡 聚-(C2_C3)-環氧烷單_、二_及三苯乙烯基苯基醚硫酸銨。 本發明調配物中表面活性劑混合物之陰離子型表面活性 劑f)與非離子型表面活性劑e)之重量比較佳介於〇.〇5:1至 10.1範圍内且尤佳介於01:1至4:1範圍内。 143575.doc 201018400 根據一尤佳實施例,組份e)採取具有不同hlb值之兩種 非離子型表面活性劑形式,特定言之一種表面活性劑e i) 及一種表面活性劑e.2),且組份£)採取陰離子型表面活性 劑形式。 通常,存在於本發明調配物中之表面活性劑的總量端視 有機植物保護劑a)及溶劑b)、匀及幻的量及其特性而定。 表面活性劑e)及f)之總量與植物保護劑a)之總量的重量比 ❹ 通常介於〇.3:1至30:1範圍内,較佳介於0.5:1至20:1範圍内 且尤佳介於1:1至7:1範圍内。表面活性劑的量通常為未經 稀釋調配物總重量之1重量%至35重量%,較佳5重量%至 25重量%,且尤佳1〇重量%至25重量0/〇。 非離子型表面活性劑e)的量通常為未經稀釋調配物總重 里之0.5重量%至30重量%,較佳4重量%至24重量%,且尤 佳5重量%至2〇重量%。 陰離子型表面活性劑f)的量通常為未經稀釋調配物總重 ^ 量之〇·5重量%至25重量%,較佳1重量%至2〇重量%,且尤 佳5重量%至15重量%。 存在於本發明調配物_之表面活性劑e)及f)及溶劑b)、 c)及d)(=有機溶劑)的總量通常端視有機植物保護劑a)之性 質及量而定。表面活性劑e) + f)加上有機溶劑b) + c) + d) 與植物保護劑a)的重量比通常介於75:1至〇.5:ι範圍内,較 佳介於50:1至1:1範圍内’且尤佳介於3〇:i至2:1範圍内。 表面活性劑加上溶劑的量通常為未經稀釋調配物總重量之 10重量%至95重量% ’較佳20重量%至85重量。/。且尤佳4〇重 143575.doc 35- 201018400 量%至7 5重量%。 根據本發明,活性物質組合物包含至少—種有機植物保 護劑。在本文中,術語「植物保護劑」應廣義理解,且不 僅包含保護植物免於被有害生物體侵襲之物質、消減損宝 植物之生物體的物質或防止損害植物之生物體生成之物 質’且亦包含影響有用植物生長(即增強或降低其生長)之 物質,包括用以改善植物健康之物質。植物保護劑之實例 包括:
殺真菌劑,即消滅植物致病真菌或降低其生長或降 低該等植物致病真菌對有用植物之感染的活性物 質; 殺昆蟲劑、殺蟎劑及殺線蟲劑,即消滅 肢動物或線蟲或減少其生成由此有效預防有二 被感染或減少該等有害生物體對植物之感染的活性 物質;
除草劑,即消滅有害植物或降低或阻止其生長之活 性物質; -生長調控劑’即促進或降低植物生長之活性物質. -安全劑’即降低或防止上述物質引起之對有用植物 之植物毒性效應的活性物質;及 肥料。 有 物 有機植物保護劑較佳盔&、,β 牧佳為低分子量有機植物保 150道爾頓至5〇〇遠膈±s 道爾頓之分子量的低分子 護劑 量有 ’即具 機化合 143575.doc • 36 - 201018400 較佳地,植物保護劑在室溫下為固體或不揮發性油,即 其在25°C下具有小於0.1毫巴之蒸氣壓。 較佳地,植物保護劑在25°C下在溶劑b)或溶劑b)、c)及 d)之混合物中之溶解度為至少1 g/Ι,尤佳至少25 g/Ι。 適宜植物保護劑之實例可自例如W· Kramer及U. Schirmer(編輯)「Modern Crop Protection Compounds」, 第 2卷,Wiley-VHC 2007 ; C.D.S. Tomlin, 「The Pesticide
V
Manual」第 13 版,British Crop Protection Council ❹ (2003);及「The Compendium of Pesticide Common
Names」,http://www.alanwood.net/pesticides/獲知。 具有殺真菌活性之活性物質的實例在下文群組A. 1至A.6 中講述: A.I.史卓比尿類(Strobilurins),例如,β坐史卓賓 (azoxystrobin)、二莫西史卓賓(dimoxystrobin)、烯肟 菌酯(enestroburin)、氟号史卓賓(fluoxastr〇bin)、克 ❼ 收欣(kresoxim-methyl)、 麥脫明諾史卓賓 (metominostrobin)、比可西史卓賓(pieoxystr〇bin)、 派拉克史卓賓(pyraclostrobin)、三氟敏(trifloxystrobin) - 、歐沙史卓賓(orysastrobin)、(2-氣-5-[l-(3-甲基苄 基氧基亞胺基)乙基]苄基)胺基甲酸曱醋、(2-氣-5-[l-(6-甲基比啶-2-基甲氧基亞胺基)乙基]苄基)胺基曱酸 曱酯、2-(鄰-(2,5-二甲基笨基氣基亞曱基)苯基)_3_甲 氧基丙烯酸曱酯; A.2 甲醯胺類,例如, 143575.doc -37- 201018400 • 曱醢苯胺類:般那拉西(benalaxyl)、精般那拉西 (benalaxyl-M)、麥鏽靈(benodanil)、萎錄靈 (carboxin)、鄰酿胺(mebenil)、滅普寧(mepronil) 、甲 °夫醯胺(fenfuram)、芬黑沙米(fenhexamid)、 氟托南尼(flutolanil)、°夫霜靈(furalaxyl)、二甲《夫 醯胺(furcarbanil)、夫南麥特(furametpyr)、滅達 樂(metalaxyl)、右滅達樂(metalaxyl-m)(精曱霜靈 (mefenoxam))、三甲0夫菌胺(methfuroxam)、嗟菌 胺(metsulfovax)、歐夫瑞絲(ofurace)、歐殺斯 Θ (oxadixyl)、氧化萎鏽靈(oxycarboxin)、0比嗔菌胺 (penthiopyrad)、D比 D南靈(pyracarbolid)、水揚苯胺 (salicylanilide)、克枯爛(tecloftalam)、西福紫麥 (thifluzamide)、替丁尼(tiadinil)、N-2-氰基苯基-3,4-二氯異噻唑-5-曱醯胺(異噻尼〇3〇^&11丨1)); • N-聯苯基醯胺類:必殺酌·(bixafen)、波斯卡利 (boscalid)、N-(4’-溴聯苯-2-基)-4-二氟曱基-2-曱 基噻唑-5-甲醯胺、N-(4’-三氟甲基聯苯-2-基)-4-二氟甲基-2-甲基噻唑-5-曱醯胺、Ν-(4·-氣-31-氟 聯苯-2-基)-4-二氟曱基-2-曱基噻唑-5-曱醯胺、Ν-(3·,4·-二氣-4-氟聯苯-2-基)-3-二氟曱基-1-曱基》比 唑-4-甲醯胺、Ν-(3’,4·,5·-三氟聯苯-2-基)-3-二氟 甲基-1-甲基D比唾-4 -甲酿胺; • 緩酸醯嗎琳類:二甲馬夫(dimethomorph)、氣馬 夫(flumorph); 143575.doc -38 - 201018400 • 苯甲蕴胺類:氟滅歐(flumetover)、氟。比菌胺 (fluopicolid)(°定苯甲醯胺(picobenzamid))、唾沙 麥(zoxamid);
• 其他曱醯胺類:卡波帕麥(carpropamid)、大克赛 美(diclocymet)、雙炔醯菌胺(mandipropamid)、 矽硫芬(silthiofam)、N-(2-(4-[3-(4-氯苯基)丙-2-炔基氧基]-3-甲氧基苯基)乙基)-2-曱烷磺醯基胺 基-3-曱基丁醯胺、N-(2-(4-[3-(4-氯苯基)丙-2-炔 基氧基]-3 -曱氧基苯基)乙基)-2 -乙烧績酿基胺基-3-曱基丁醯胺; A. 3 · °坐類,例如, • (bromuconazole)、環克口圭(cyproconazole)、地芬 康唾(difenoconazole)、烯°坐醇(diniconazole)、安 尼康 °^(enilconazole)、環氧康 ^(epoxiconazole)、 芬布康唾(fenbuconazole)、護石夕得(flusilazol)、 氟喧康唾(fluquinconazole)、護汰芬、六康口坐 (hexaconazole)、醯胺0坐(imibenconazole)、種菌 唾(ipconazole)、麥康 °坐(metconazole)、麥環丁尼 (myclobutanil)、潘康嗤(penconazole)、普克利 (propiconazole)、撲硫康0坐(prothioconazole)、石夕 氣0坐(simeconazole)、得克利(tebuconazole)、四 凯利(tetraconazole)、三泰隆(triadimenol)、三泰 芬(triadimefon)、三替康唾(triticonazole); • 11米唾類:賽嗤法米(cyazofamid)、依滅列 143575.doc -39- 201018400 (imazalil)、稻痕 S旨(pefurazoate)、撲克拉 (prochloraz)、三氟0米0坐(triflumizole); • 苯并咪°坐類:免賴得(benomyl)、多菌靈 (carbendazim)、夫伯達 β坐(fuberidazole)、腐絕 (thiabendazole); • 其他:衣沙布山(ethaboxam) 、 土菌靈 (etridiazole)、惡黴靈(hymexazol); A. 4.含氮雜環化合物,例如, • °比咬類:扶吉胺(fuazinam)、比利芬羅 (pyrifenox)、3-[5-(4-氯苯基)-2,3-二曱基異噁唑 - 3 -基]-π定, • 嘴咬類:乙°密紛績酸醋(bupirimate)、賽普洛 (cyprodinil)、鳴菌膝(ferimzone)、芬瑞莫 (fenarimol)、米潘尼比林(mepanipyrim)、紐阿利 莫(nuarimol)、比利美沙尼(pyrimethanil); • 六氫°比唤類:賽福寧(triforine); •。比σ各類:氟二惡尼(fludioxonil)、芬比克隆尼 (fenpiclonil); • 嗎琳類:阿迪莫夫(aldimorph)、嗎菌靈 (dodemorph)、芬普福(fenpropimorph)、三得芬 (tridemorph); • 二叛醯亞胺類:依普同(iprodione)、撲滅寧 (procymidone)、免克寧(vinclozolin); •其他:S-曱基阿西本0坐(acibenzolar-S-methyl)、 143575.doc -40- 201018400 敵菌靈(anilazine)、蓋普丹(captan)、蓋它福 (captafol)、邁隆(dazomet)、大克美秦(diclomezin) 、芬咢尼(fenoxanil)、福爾培(folpet)、芬普比定 (fenpropidin)、泛惡同(famoxadon)、芬納米同 (fenamidon)、辛 α塞酮(octhilinone)、撲殺熱 (probenazole)、普奎那兹(proquinazid)、百快隆 (pyroquilon)、奎諾克西芬(quinoxyfen)、三賽口坐 (tricyclazole)、5 -氯-7-(4-曱基六氫0比咬-1-基)-6-(2,4,6-三氟苯基)-[1,2,4]三唑并[l,5-a]嘧啶、2-丁 氧基-6-碘代-3-丙基咣烯-4-酮、N,N-二甲基-3-(3-漠-6 -氣-2-甲基0引〇朵-1-石黃酿基)-[1,2,4]二唾-1-續 醯胺; A.5.
胺基曱酸酯類及二硫代胺基甲酸酯類,例如, • 二硫代胺基甲酸酯類:富爾邦(ferbam)、錳粉 克(mancozeb)、猛乃浦(maneb)、免得爛 (metiram)、美坦(metam)、曱基辞乃浦 (propineb)、得恩地(thiram)、辞乃浦(zineb)、 益穗(ziram); • 胺基曱酸酯類:二乙芬卡(diethofencarb)、氟 本賽夫利卡(flubenthiavalicarb)、衣普法利卡 (iprovalicarb)、普潘莫卡(propamocarb)、3-(4-亂苯基)-3-(2 -異丙氣基幾基胺基-3-甲基丁酿基 胺基)丙酸甲酯、N-(l-(l-(4-氰基苯基)乙磺醯 基)丁-2-基)胺基甲酸4-氟苯基酯; 143575.doc -41 - 201018400 A.6.其他殺真菌劑,例如, •脈類:多寧(dodine)、亞胺歐它丁(iminoctadine)、 雙胍辛胺(guazatine); • 抗生素類:喜賜黴素(kasugamycin)、保粒黴素 (polyoxin)、鏈黴素(streptomycin)、維利黴素 (validamycin A); •有機金屬化合物類:三苯基錫鹽; • 含硫雜環化合物:亞賜圃(isoprothiolane)、腈硫 酉昆(dithianone); • 有機填化合物:護粒松(edifenphos)、福賽得 (fosetyl)、福賽得紹(fosetyl-aluminum)、丙基喜 樂松(iprobenfos)、白粉松(pyrazophos)或脫克松 (tolclofos-methyl); • 有機氣化合物:甲基多保淨(thiophanate-methyl)、四氯異苯腈(chlorothalonil)、益發靈 (dichlofluanid)、對曱抑菌靈(tolylfluanid)、績菌 胺(flusulfamide)、四氣苯酿(phthalide)、六氣苯 (hexachlorobenzene)、賓克隆(pencycuron)、奎脫 辛(quintozene); • 琐基苯基衍生物:百滿克(binapacryl)、白粉克 (dinocap)、大脫蜗(dinobuton); • 其他:螺惡胺(spiroxamine)、賽扶芬納米 (cyflufenamid)、西莫生尼(cymoxanil)、美查芬隆 (metrafenon) 〇 143575.doc -42- 201018400 具有殺昆蟲、殺蟎及/或殺線蟲活性之活性物質的實例 在群組B.1至B.24中講述:
B.I.有機(硫代)磷酸酯類:高滅磷(acephate)、亞滅松 (azamethiphos)、益棉填(azinphos-ethyl)、保棉填 (azinphos-methyl)、氯氧磷(chlorethoxyfos)、氣芬填 (chlorfenvinphos)、氣甲稱(chlormephos)、毒死蜱 (chlorpyrifos)、甲基毒死碑(chlorpyrifos-methyl)、 庫馬墻(coumaphos)、殺填腈(cyanophos)、硫趕式曱 基内吸磷(demeton-S-methyl)、敵匹硫填(diazinon)、 敵敵畏(dichlorvos) (DDVP)、百治麟(dicrotophos)、 樂果(dimethoate)、甲基毒蟲畏(dimethylvinphos)、 乙拌填(disulfoton)、EPN、乙硫構(ethion)、丙線破 (ethoprophos)、胺續填(famphur)、苯線墙 (fenamiphos)、殺堪松(fenitrothion)、倍硫構 (fenthion)、氟定菌鱗(flupyrazophos)、0塞唾麟 (fosthiazate)、庚烯填(heptenophos)、°惡嗤碌 (isoxathion)、馬拉硫填(malathion)、滅財填 (mecarbam)、甲胺填(methamidophos)、殺撲構 (methidathion)、甲基巴拉松(methyl-parathion)、速 滅填(mevinphos)、久效填(monocrotophos)、三演填 (naled)、氧樂果(omethoate)、亞碉1 填(oxydemeton-methyl)、雙氧雄(paraoxon)、巴拉松(parathion)、甲 基巴拉松(parathion-methyl)、稻豐散(phenthoate)、 曱拌鱗(phorate)、伏殺礙(phosalone)、亞胺硫填 143575.doc -43- 201018400
(phosmet)、填胺(phosphamidon)、將硫璃(phoxim)、 甲基喊咬麟(pirimiphos-methyi)、丙漠填(profenofos) 、胺丙畏(propetamphos)、丙硫鱗(prothiofos)、0比0坐 硫鱗(pyraclofos)、必芬松(pyridaphenthion)、喧惡淋 (quinalphos)、治埃鱗(sulfotep)、殺普松(sulprophos) 、丁 基嘴咬填(tebupirimfos)、替美填(temephos)、特 丁填(terbufos)、司替羅填(tetrachlorvinphos)、甲基 乙拌鱗(thiometon)、三。坐磷(triazophos)、三氯松 (trichlorfon)、财滅多(vamidothion); ❹ B.2.胺基甲酸酯類:涕滅威(aldicarb)、棉鈴威 (alanycarb)、惡蟲威(bendiocarb)、丙硫克百威 (benfuracarb)、丁叉威(butocarboxim)、丁 酮颯威 (butoxycarboxim)、胺曱萘(carbaryl)、蟲蜗威 (carbofuran)、丁硫克百威(carbosulfan)、乙硫苯威 (ethiofencarb)、仲 丁威(fenobucarb)、伐蟲脒 (formetanate)、0夫線威(furathiocarb)、異丙威(isoprocarb) 、滅蟲威(methiocarb)、滅多蟲(methomyl)、速滅威 (metolcarb)、草胺醯(oxamyl)、抗財威(pirimicarb)、 安丹(propoxur)、硫雙威(thiodicarb)、久效威 (thiofanox)、混殺威(trimethacarb)、XMC、滅殺威 (xylylcarb)、唾財威(triazamate); B.3.擬除蟲菊醋類:I丙菊醋(acrinathrin)、丙烯除蟲菊 (allethrin)、右旋-順-反丙烯除蟲菊、右旋-反丙稀除 蟲菊、聯苯菊醋(bifenthrin)、反丙稀除蟲菊 143575.doc -44 - 201018400 • (bioallethrin)、S-環戊烯基反丙烯除蟲菊、除蟲菊酯 (bioresmethrin)、乙氰菊酯(cyci〇prothrin)、賽扶寧 (eyfluthrin)、β-賽扶寧、賽洛寧(cyhalothrin)、λ-赛 洛寧、γ-赛洛寧、赛滅寧(Cypermethrin)、α-賽減 寧、β-賽滅寧、Θ-賽滅寧、ζ_赛滅寧、苯醚氰菊酯 (cyphenothrin)、溴氰菊酯(deltamethrin)、右旋烯炔 菊酯(empenthrin)、伊芬化利(esfenvalerate)、依芬普 司(etofenprox)、曱氰菊醋(fenpropathrin)、芬化利 (fenvalerate)、護赛寧(flucythrinate)、氟氯苯菊 6旨 (flumethrin)、τ-福化利(tau-fluvalinate)、苄瞒醚 (halfenprox)、依普寧(imiprothrin)、美特寧(metofluthrin) 、撲滅司林(permethrin)、苯氧司林(phenothrin)、快 稀菊酯(prallethrin)、丙氟菊醋(profluthrin)、除蟲菊 素(pyrethrin)(除蟲菊(pyrethrum))、苄吱菊酯 (resmethrin)、RU 15525、西拉福芬(silafluofen)、七 • 氟菊醋(tefluthrin)、四甲司林(tetramethrin)、四漠菊 醋(tralomethrin)、四氟苯菊醋(transfluthrin)、ZXI 8901 ; Β.4. • 保幼激素模擬物:稀蟲乙酯(hydroprene)、丙諾保幼 素(kinoprene)、甲氧普林(methopren)、芬諾西克 (fenoxycarb)、比普西芬(pyriproxyfen); Β.5. 終驗受體激動劑/拮抗劑化合物:咬轰脒 (acetamiprid)、殺蟲續(bensultap)、殺埃丹(cartap-hydrochloride)、可尼丁(clothianidin)、達特南 143575.doc ·45· 201018400 (dinotefuran)、n比蟲淋(imidacloprid)、赛速安 (thiamethoxam)、尼藤 °比藍(nitenpyram)、尼古丁 (nicotine)、賜諾殺(spinosad)(變構性激動劑)、斯0比 特安(spinetoram)、β塞蟲琳(thiacloprid)、殺蟲環 (thiocyclam)、殺蟲雙(thiosultap-sodium)及AKD1022。 B.6. GABA受控氣離子通道拮抗劑化合物:氯丹 (chlordan)、安殺番(endosulfan)、γ-HCH(靈丹 (lindan))、乙醯蟲腈(acetoprole)、伊希普(ethiprole)、 費普尼(Hpronil)、比氟普魯(pyrafluprole)、比普魯 (pyriprole)、凡尼力普魯(vaniliprole); B.7.氯離子通道激活劑:阿巴克丁(abamectin)、伊曼美 丁苯曱酸鹽(emamectin benzoate)、密滅汀(milbemectin) 、萊培菌素(lepimectin); B.8. METI I化合物:啥瞒鍵(fenazaquin)、嗅蜗醋 (fenpyroximate)、喊瞒醚(pyrimidifen)、建蜗靈 (pyridaben)、D比瞒胺(tebufenpyrad)、°坐蟲醯胺 (tolfenpyrad)、氟驗瑞姆(flufenerim)、魚藤 _ (rotenone); B.9. METI II及III化合物:阿色奎西(acequinocyl)、氟克 瑞姆(fluaeyprim)、經甲隆(hydramethylnon); B.10.氧化構酸化之解偶聯劑:克芬那比(chlorfenapyr)、 DNOC ; B. 11.氧化鱗酸化抑制劑:三唾錫(azocyclotin)、三環錫 (cyhexatin)、丁醚腺(diafenthiuron)、苯丁錫 143575.doc -46- 201018400 (fenbutatin oxide)、炔蜗特(propargit)、四氣殺蜗礙 (tetradifon); B.12.蜆皮抑制劑:環丙馬秦(cyromazin)、可芬諾 (chromafenozide)、鹵芬載(halofenozide)、曱氧芬載 (methoxyfenozide)、得布芬載(tebufenozide); B.13.增效劑:胡椒基丁.醚(piperonyl butoxide)、脫葉鱗 (tribufos); B.I4.納通道阻斷劑:引多殺克(indoxacarb)、美氟綜 ❹ (metaflumizon); B.I5.選擇性拒食劑:冰晶石(crylotie)、比美卓秦 (pymetrozine)、氟咬蟲醯胺(flonicamid); Β·16·蜗類生長抑制劑:克芬蜗(clofentezine)、合赛多 (hexythiazox)、伊妥 °惡°坐(etoxazole); B.17.幾丁質合成抑制劑:布芬淨(buprofezin)、雙三氟蟲 脲(bistrifluron)、敗 °定脲(chlorfluazuron)、二氟苯隆 _ (diflubenzuron)、氟環腺(Hucycloxuron)、氟芬隆 (flufenoxuron)、六伏隆(hexaflumuron)、氣芬奴隆 (lufenuron)、諾華隆(novaluron)、多氟脲(noviflumuron) 、得福隆(teflubenzuron)、殺蟲隆(triflumuron); Β· 1 8.脂質生物合成抑制劑:螺二克芬(spirodiclofen)、螺 美芬(spiromesifen)、螺蟲乙醋(spirotetramate); Β· 19.章魚胺能激動劑(octopaminergic agonists):三亞瞒 (amitraz); B.2〇.蘭尼鹼(ryanodine)受體調節劑:氟蟲醯胺 143575.doc •47- 201018400 (flubendiamide); B.21·其他:醯胺l米特(amidoflumet)、本氣嗟 (benclothiaz)、苯瞒特(benzoximate)、畢务載 (bifenazate)、漠蜗醋(bromopropylate)、賽謹若紛 (cyenopyrafen)、丁氟蜗酯(cyflumetofen)、滅滿猛 (quinomethionate) ' 開樂散(dicofol)、氟乙酸酯 (fluoroacetate)、膦(phosphine)、咬蟲丙醚(pyridalyl) 、比氟喧膝(pyrifluquinazone)、有機硫化合物、績薩 氟(8111€〇乂3£1〇]*)、4-丁-2-炔基氧基-6-(3,5-二甲基-六 氫°比咬-1-基)-2 -氟-嘴唆、3 -苯曱醯基胺基-N-[2,6-二 甲基-4-(1,2,2,2-四氟-1-三氟甲基·乙基)_苯基]-2-氟-苯曱醯胺、4-[5-(3,5-二氣_苯基)_5-三氟曱基-4,5-二 氫-異噁唑-3-基]-2-甲基-N-吡啶-2-基甲基-苯甲醯 胺、4-[5-(3,5-二氣-苯基)_5_三氟曱基_4,5_二氫·異噁 嗤-3-基]-2-甲基-N-(2,2,2-三氟-乙基)_苯甲醯胺、4-[5-(3,5-二氣-苯基)_5_三氟甲基_4,5_二氫-異噁唑_3-基]-2-曱基-N-嗟唑-2-基甲基-苯曱醯胺、4-[5-(3,5-二 氣-苯基)-5-三氟甲基_4,5_二氫-異噁唑_3_基]_2_甲基_ N-(四氫-呋喃-2-基甲基)_苯曱醯胺、 4-{[(6-溴吡啶基)曱基](2_氟乙基)胺基}呋喃_ 2(5H)-酮、 4-{[(6-氟吼啶-3·基)甲基](2,2_二氟乙基)胺基}呋喃_ 2(5H)-酮、 4-{[(2-氣-1,3-噻〇坐_5_基)甲基](2_乾乙基)胺基卜夫喃- 143575.doc -48 - 201018400 2(5H)-酮、 4·{[(6-氯》比啶-3-基)甲基](2-氟乙基)胺基}呋喃-2(5H)-酮、 4-{[(6-氯吡啶-3-基)甲基](2,2-二氟乙基)胺基}呋喃-2(5H)-酮、 4_{[(6-氯-5-氟吡啶-3-基)甲基](甲基)胺基}呋喃-2(5H)-嗣、
4-{[(5,6-二氯α比啶_3_基)甲基](2_氟乙基)胺基}呋喃· 2(5Η)-酮、 4_{[(6-氣_5_氟咕啶-3-基)曱基](環丙基)胺基}呋喃-2(5Η)-酮、 4-{[(6-氯。比啶_3_基)甲基](環丙基)胺基}呋喃-2(5Η)-酮、 ‘{[…-氯吼啶-:^基丨甲基从曱基彡胺基丨呋喃·“5^)- 酮、 環丙烷乙酸 l,l'-[(3S,4R,4aR,6S,6aS,12R,12aS,12bS)-4-[[(2-環丙基乙醯基)氧基]甲基]_i,3,4,4a,5,6,6a,12, 12a,12b-十氫-12-羥基_4,6a,12b-三甲基-11-側氧基-9-(3-吡啶基)-2Η,11Η-萘并[2,l-b]吡喃並[3,4-e]吡喃-3,6-二基]6 旨、 8-(2-環丙基甲氧基-4-曱基-苯氧基)-3-(6-甲基-噠嗪-3-基)-3-氮雜-二環[3.2.1]辛烷 6.22.>1-11'-2,2-二鹵基-1-尺|'-環-丙烷曱醯胺-2-(2,6-二氣-α,α,α-三氟-對曱苯基)腙或N-R'-2,2-二-R·"-丙醯胺-2- 143575.doc •49· 201018400 (2,6-二氣-α,α,α-三氟-對曱苯基)_腙,其中r*代表甲 基或乙基,鹵基代表氯或溴,R"代表氫或曱基,且 R"'代表曱基或乙基; B.23.胺基苯醯胺(Anthranilamide)化合物:氣斯胺普 (chloranthraniliprole)、氰尼利普(cyantraniliprole)、 5->臭-2-(3 -氣-0比淀-2 -基)-211-0比〇坐-3 -曱酸[4 -氣基-2-(1-環丙基-乙基胺曱醯基)-6-甲基-苯基]-醯胺、 5 -溴-2-(3 -氣-0比咬-2 -基)-2H- 0比0坐-3-甲酸[2-氣-4 -氣 基-6-(1-環丙基-乙基胺甲醯基)-苯基]-醯胺、 5-溴-2-(3-氣-吡啶-2-基)-2H-吡唑-3 -曱酸[2-溴-4-氰 基-6-(1-環丙基-己基胺甲醯基)-苯基]-醯胺、 5- 溴-2-(3-氣-吡啶-2-基)-2H-吡唑-3-曱酸[2-溴-4-氯- 6- (1-環丙基-乙基胺甲醯基)-苯基]-趨胺、 5-溴-2-(3-氣-吡啶-2-基)-2H-吡唑-3-曱酸[2,4-二氣-6-(1-環丙基-乙基胺甲醯基)-苯基]•醯按、 5-溴-2-(3-氣-吡啶-2-基)_2H-吡唑-3 -甲酸[4-氣-2-(1-環丙基-乙基胺甲醯基)-6-曱基-苯基]-醯胺 B.24.丙二腈化合物:CF2HCF2CF2CF2CH2C(CN)2CH2CH2CF3 (2-(2,2,3,3,4,4,5,5-八氟戊基)-2-(3,3,3-三氟丙基)丙 二腈)、CF3(CH2)2C(CN)2CH2(CF2)5CF2H (2-(2,2,3,3, 4,4,5,5,6,6,7,7-十二氟庚基)-2-(3,3,5-三氟丙基)丙二 腈)、CF3(CH2)2C(CN)2(CH2)2C(CF3)2F (2-(3,4,4,4-四 氟-3-三氟曱基丁基)-2-(3,3,3-三氟丙基)丙二腈)、 CF3(CH2)2C(CN)2(CH2)2(CF2)3CF3 (2-〔3,3,4,4,5,5,6,6,6- 143575.doc -50- 201018400 九氟-己基)-2-(3,3,3-三氟丙基)丙二腈)、 CF2H(CF2)3CH2C(CN)2CH2(CF2)3CF2H (2,2-雙-(2,2,3, 3.4.4.5.5- 八氟戊基)丙二腈)、CF3(CH2)2C(CN)2CH2(CF2)3CF3 (2-(2,2,3,3,4,4,5,5,5-九氟戊基)-2-(3,3,3-三氟丙基)丙 二腈)、CF3(CF2)2CH2C(CN)2CH2(CF2)3CF2H(2-(2,2, 3,3,4,4,4-七氟丁基)-2-(2,2,3,3,4,4,5,5-八氟戊基)丙 二腈)、CF3CF2CH2C(CN)2CH2(CF2)3CF2H(2-(2,2,3,3, 4.4.5.5- 八氟戊基)-2-(2,2,3,3,3-五氟丙基)丙二腈)、 CF2HCF2CF2CF2CH2C(CN)2CH2CH2CF2CF3(2-(2,2,3, 3.4.4.5.5- 八氟戊基)-2-(3,3,4,4,4-五氟丁基)丙二腈)、 CF3(CH2)2C(CN)2CH2(CF2)3CF2H(2-(2,2,3,3,4,4,5,5-八氟戊基)-2-(3,3,3-三氟丁基)丙二腈); 群組B之市售化合物列示於(例如)「The Pesticide Manual」,第 13 版,British Crop Protection Council (2003)及其他出版物中。 萊培菌素係自Agro Project(PJB Publications有限公司, 2004年11月)獲知。本氣噻及其合成已闡述於EP-A1 454621中。殺撲磷及雙氧磷及其合成已闡述於Farm Chemicals Handbook(第 88 卷,Meister 出版公司,2001) 中。乙醯蟲腈及其合成已闡述於WO 98/28277中。美氟综 及其合成已闡述於EP-A1 462 456中。I定菌填 (Flupyrazofos)已闡述於 Pesticide Science 54(1988,第 237-243頁)及美國專利第4822779號中。比氟普魯及其合成已 闡述於日本專利第20〇2193709號及WO 01/00614中。比普 143575.doc •51· 201018400 魯及其合成已闡述於WO 98/45274及美國專利第6,335,357 號中。醯胺氟米特及其合成已闡述於美國專利第6,221,890 號及日本專利第21010907號中。氟酚瑞姆及其合成已闡述 於 WO 03/007717 及 WO 03/007718 中。AKD 1022 及其合成 已闡述於美國專利第6300348號中。氣斯胺普已闡述於WO 01/70671、WO 03/015519 及 WO 05/1 18552 中。氰尼利普已 闡述於 WO 01/70671、WO 04/067528 及 WO 05/118552 中。
其他胺基苯酿胺衍生物已闡述於WO 01/70671、WO 04/067528及WO 05/118552中。丁氟蟎酯及其合成已闡述 參 於WO 04/080180中。胺基喹唑啉酮化合物比氟喹腙已闡述 於EP A 109 7932中。諸如磺薩氟(sufloxaflor)及其類似物 等磺醯亞胺衍生物(包括其合成)已闡述於WO 2006/060029 及2007/149 134中。炔基醚化合物已闡述於例如日本專利 第2006 13 1529號中。有機硫化合物已闡述於WO 07/060839 中。丙二腈化合物已闡述於WO 02/089579、WO 02/090320 、 WO 02/090321 、 WO 04/006677 、 WO 05/068423、WO 05/068432及 WO 05/063694 中。 ❹ 具有除草活性之活性物質的實例在群組C.1至C.15中講 述: C. 1 脂質生物合成抑制劑,例如,氣禾靈(chlorazifop)、 炔草酯(clodinafop)、2-(4-(4-氯苯氧基)苯氧基> 丙酸 (clofop)、丁基賽伏草(cyhalofop)、禾草靈(diclofop)、 °惡。圭禾草靈(fenoxaprop)、精°惡°坐禾草靈(fenoxaprop-p)、0坐禾草靈酸(fenthiaprop)、。比氟禾尊靈 143575.doc -52- 201018400
(fluazifop)、精。比氟禾草靈(fluazifop-P)、氟°比禾靈 (haloxyfop)、精氣 β比禾靈(haloxyfop-P)、異 °惡草醚 (isoxapyrifop)、°惡哇醯草胺(metamifop)、普拔草 (propaquizafop)、啥禾靈(quizalofop)、精喧禾靈 (quizalofop-P)、三氟殺草(trifop)、禾草滅 (alloxydim)、丁 苯草酮(butroxydim)、稀草酮 (clethodim)、環丙殺草(cloproxydim)、環殺草 (cycloxydim)、環苯草酮(profoxydim)、西殺草 (sethoxydim)、得殺草(tepraloxydim)、三甲苯草嗣 (tralkoxydim) 、 丁草特(butylate)、草滅特 (cycloate)、燕麥敵(di-allate)、派草丹 (dimepiperate)、EPTC、戊草丹(esprocarb)、抑草威 (ethiolate)、異普利特(isopolinate)、滅賜苯克 (methiobencarb)、禾草歒(molinate)、坪草丹(orbencarb) 、克草敵(pebulate)、苄草丹(prosulfocarb)、草克死 (sulf-allate)、禾草丹(thiobencarb)、仲草丹(tiocarbazil) 、野麥畏(tri-allate)、滅草敵(vernolate)、β夫草黃 (benfuresate)、乙0夫草黃(ethofumesat)及地散鱗 (bensulid); C.2 ALS抑制劑,例如,醯痛續隆(amidosulfuron)、四唾 0密續隆(azimsulfuron)、》密續隆酸(bensulfuron)、氯嘯 續隆(chlorimuron)、氣續隆(chlorsulfuron)、西速隆 (cinosulfuron)、環確隆(cyclosulfamuron)、胺苯續隆 (ethametsulfuron)、亞速隆(ethoxysulfuron)、伏速隆 143575.doc -53· 201018400
(flazasulfuron)、氟咬0^ 績隆(flupyrsulfuron)、酿胺 續隆(foramsulfuron)、氯"比》密確隆(halosulfuron)、依 速隆(imazosulfuron)、蛾確隆(iodosulfuron)、甲基二 磺隆(mesosulfuron)、曱績隆(metsulfuron)、煙嘴橫 隆(nicosulfuron)、環氧嘴續隆(oxasulfuron)、氣喊續 隆(primisulfuron)、三敗丙績隆(prosulfuron)、百速 隆(pyrazosulfuron)、玉嘴績隆(rimsulfuron)、嗜確隆 (sulfometuron)、績醯績隆(sulfosulfuron)、售罐隆 (thifensulfuron)、謎苯確隆(triasulfuron)、苯罐隆 (tribenuron)、三氣咬確隆(trifloxysulfuron)、氟胺橫 隆(triflusulfuron)、三氟曱績隆(tritosulfuron)、米草 酸(imazamethabenz)、曱氧咪草煙(imazamox)、甲基 口米草煙(imazapic)、依滅草(imazapyr)、滅草啥 (imazaquin)、°米°坐乙煙酸(imazethapyr)、氣S旨確草胺 (cloransulam)、雙氣項草胺(diclosulam)、雙敦續草 胺(florasulam)、唾啦續草胺(flumetsulam)、碍草0坐 胺(metosulam)、五氟績草胺(penoxsulam)、雙草醚 (bispyribac)、°密草喊(pyriminobac)、丙苯績隆 (propoxycarbazone)、氟酮石黃隆(flucarbazone)、嘴咬 月亏草鍵(pyribenzoxim)、環醋草醚(pyriftalid)及密草 硫 _(pyrithiobac); C.3 光合成抑制劑,例如,莠去通(atraton)、阿特拉嗪 (atrazine)、莠滅淨(ametryn)、疊氮淨(aziprotryn)、 氰乃淨(cyanazine)、氰草淨(cyanatryn)、可樂津 143575.doc -54- 201018400
(chlorazine)、環丙津(cyprazin)、地蔓盡(desmetryn)、 異戊乙淨(dimethametryn)、異丙淨(dipropetryn)、甘 草津(eglinazine)、抑草律(ipazine)、滅筹津 (mesoprazine)、謎草通(methometon)、蓋草津 (methoprotryn)、環丙氰津(procyazine)、甘撲津 (proglinazine)、撲滅通(prometon)、撲草淨 (prometryn)、撲滅津(propazine)、另丁津 (sebuthylazine)、仲丁通(secbumeton)、草滅淨 (simazine)、西瑪通(simeton)、西草淨(simetryn)、甲 氧去草淨(terbumeton)、草淨津(terbuthylazine)、去 草淨(terbutryn)、草達津(trietazine)、阿美酮 (ametridione)、阿米布嗪(amibuzine)、環1秦酮 (hexazinon)、丁 嘹草酮(isomethiozine)、苯嗓草酮 (metamitron)、嗪草酮(metribuzine)、除草定 (bromacil)、異草定(isocil)、環草定(lenacil)、特草 定(terbacil)、漠莠敏(brompyrazon)、殺草敏 (chloridazon)、草噠酮(dimidazon)、甜菜安 (desmedipham)、棉胺寧(phenisopham)、甜菜寧 (phenmedipham)、甜菜寧-乙 S旨(phenmedipham-ethyl)、售草隆(benzthiazuron)、丁嗟隆(buthiuron)、 績售隆(ethidimuron)、異°惡隆(isouron)、甲苯嗟隆 (methabenzthiazuron)、單異"惡隆(monoisouron)、特 丁 嗟草隆(tebuthiuron)、嘆氟隆(thiazafluron)、阿尼 隆(anisuron)、播土隆(buturon)、氯溴隆 143575.doc -55- 201018400 (chlortromuron)、氣乙隆(chloreturon)、綠麥隆 (chlorotoluron)、枯草隆(chloroxuron)、枯莠隆 (difenoxuron) 、口惡♦隆(dimefuron)、敵草隆 (diuron)、非草隆(fenuron)、伏草隆(fluometuron)、 氟硫隆(fluothiuron)、異丙隆(isoproturon)、利榖隆 (linuron)、滅草恒(methiuron)、甲氧苯草隆 (metobenzuron)、漠榖隆(metobromuron)、甲氧隆 (metoxuron)、綠穀隆(monolinuron)、滅草隆 (monu ron)、草不隆(neburon)、對氟隆(parafluron)、 醯草蔭:(phenobenzuron)、環草隆(siduron)、四氟隆 (tetrafluron)、嘆苯隆(thidiazuron)、牧草快 (cyperquat)、二乙草快(diethamquat)、野燕枯 (difenzoquat)、敵草快(diquat)、伐草快 (morfamquat)、百草枯(paraquat)、除草溴 (bromobonil)、漠苯腈(bromoxynil)、經敵草腈 (chloroxynil)、除草块(iodobonil)、埃苯腈 (ioxyail)、胺0坐草酮(amicarbazone)、溴齡將 (bromofenoxim)、氟曱 °l: (flumezine)、滅草定 (methazole)、滅草松(bentazone)、敵稗(propanil)、 甲氯盛草胺(pentanochlor)、達草特(pyridate)及達草 伏(pyridafol); C.4 卟啉原IX氧化酶抑制劑,例如,亞喜芬 (aciflmorfen)、必芬諾(bifenox)、甲氧除草趟 (chloinethoxyfen)、全滅草(chlornitrofen)、氣氟草 ϋ -56-
143575.doc 201018400 (ethoxyfen)、三氟石肖草醚(fluorodifen)、乙缓氟草醚 (fluoroglycofen)、氟除草 il(fluoronitrofen)、敦績胺 草醚(fomesafen)、氧草醚(furyloxyfen)、路薩芬 (halosafen)、乳 II 禾草靈(lactofen)、護穀 (nitrofen)、三氟曱草醚(nitrofluorfen)、複祿芬 (oxyfluorfen)、異丙草醋(fluazolate)、D比草鍵 (pyraflufen)、°引嗓酮草醋(cinidonethyl)、敗烯草酸 (flumiclorac)、丙炔氟草胺(flumioxazin)、炔草胺 (flumipropyn)、氟售乙草 S旨(fluthiacet)、°塞二嗤草胺 (thidiazimin)、樂滅草(oxadiazon)、丙块 °惡草酮 (oxadiargyl)、草芬定(azafenidin)、。坐酮草 S旨 (carfentrazone)、甲續草胺(sulfentrazone)、環戊 °惡草 酮(pentoxazone)、雙苯嘴草酮(benzfendizone)、氟丙 口密草g旨(butafenacil)、雙°坐草腈(pyraclonil)、氟唾草 胺(profluazole)、氣建°秦草酯(flufenpyr)、氟°密°定草 酯(flupropacil)、°比氣草胺(nipyraclofen)及伊尼普米 (etnipromid); C.5 漂白除草劑,例如,二甲達草伏(metflurazon)、氟草 敏(norflurazon)、氟草胺(flufenican)、°比氟醯草胺 (diflufenican)、氟 °比酿草胺(picolinafen)、氟 丁草胺 (beflubutamid)、氟咬草酮(fluridone)、氟洛草酮 (flurochloridone)、°夫草酮(flurtamone)、曱基確草酮 (mesotrione)、績草酿I (sulcotrione)、異 °惡氣草酮 (isoxachlortole)、異。惡。坐草酮(isoxaflutole)、π比草酮 143575.doc -57- 201018400 (benzofenap)、,草吐(pyraz〇iynate)、匹峻芬 (pyrazoxyfen)、篆并雙環酮(benz〇biCyCi〇n)、殺草強 (amitrole)、可滅雖(ci〇maz〇ne)、苯草越(aci〇nifen)、 4-(3-三氟曱基笨氧基三氟曱基苯基)嘧啶及式 II之經3-雜環基取代之苯甲醢基衍生物(參見w〇
96/26202、WO 97/41116、WO 97/41117 及 WO 97/41118)
R8、R10係氫、鹵f、C】-C6-烧基、CVCV鹵代烷基、 CVCV烧氧基、鹵代烷氧基、CVC6-烷基硫 基、c^-cv烧基亞磺醯基或Ci_C6_烷基磺醯基; R9係選自由下列組成之群之雜環基團:噻唑_2_ 基、噻唑-4-基、噻唑_5_基、異噁唑_3_基、異噁 唾-4-基、異噁唑-5-基、4,5-二氫異噁唑-3-基、0 4,5-—氫異惡吐-4-基及4,5_二氫異n惡嗤_5_基,上 述九個基團T未經取代或經鹵素、Cl_c4-烷基、
Ci-C4-烷氧基、(VC4-幽代烷基、c】-C4-鹵代烷氧 基或C!-C4_燒基硫基單取代或多取代,例如單取 代、—取代、二取代或四取代; R"係氫、鹵素或Ci-CV燒基; R12烷基; -58- 143575.doc 201018400 C.6 R12係^-匕-烷基; R13係氫或CVCV烷基。 EPSP合成酶抑制劑,例如,草甘膦(glyphosate); C.7 麵胺醯胺合成酶抑制劑,例如,草錢膦(glufosinate) 及雙丙胺膦(bilanaphos); C.8 DHP合成酶抑制劑,例如,續草靈(asulam); C.9 有絲分裂抑制劑,例如,倍尼芬(benfluralin)、比達 參 寧(butralin)、撻乃安(dinitramin)、丁 氟消草 (ethalfluralin)、氣乙氟靈(fluchloralin)、異丙樂靈 (isopropalin)、曱丙樂靈(methalpropalin)、續樂靈 (nitralin)、歐拉靈(oryzalin)、施得圃(pendimethalin) 、氨氟樂靈(prodiamin)、卡樂施(profluralin)、氟樂 靈(trifluralin)、甲基胺草碌(amiprofosmethyl)、丁胺 璘(butamifos)、汰硫草(dithiopyr)、嘆草咬(thiazopyr) 、炔苯草胺(propyzamide)、牧草胺(tebutam)、大克 草(chlorthal)、雙草胺(carbetamide)、氣炔靈 (chlorbufam)、氣苯胺靈(chlorpropham)及苯胺靈 (propham); C.10 VLCFA抑制劑,例如,乙草胺(acetochlor)、拉草 (alachlor)、丁 基拉草(butachlor)、丁 烯草胺 (butenachlor)、異 丁草胺(delachlor)、乙甲草胺 (diethatyl)、二甲草胺(dimethachlor)、二甲吩草胺 (dimethenamid)、精二甲吩草胺(dimethenamid-P)、 滅草胺(metazachlor)、莫多草(metolachlor)、左旋莫 143575.doc -59- 201018400 多草(S-metolaehlor)、普拉萆(pretilachlor)、毒草胺 (propachlor)、異丙草胺(propisochlor)、丙快草胺 (prynachlor)、特 丁草胺(terbuchlor)、甲氧草胺 (thenylchlor)、二甲苯草胺(zxylachlor)、二丙稀草胺 (allidochlor)、CDEA、伊普納茲(epronaz)、大芬滅 (diphenamide)、滅落脫(napropamide)、萘丙胺 (naproanilide)、稀草胺(pethoxamid)、氟草胺 (flufenacet)、滅芬草(mefenacet)、四 °坐酮 (fentrazamide)、莎稗填(anilofos)、草填(piperophos) 、咬草胺(cafenstrol)、草朗(indanofan)及滅草環 (tridiphane); C.11纖維素生物合成抑制劑,例如,敵草腈 (dichlobenil)、草克樂(chlorthiamid)、異 °惡草胺 (isoxaben)及氟胺草唾(flupoxzam); C.12解偶聯劑除草劑,例如,地樂特(dinofenate)、丙石肖 酌'(dinoprop)、戊硝紛(dinosam)、達諾殺(dinoseb)、 特樂酴(dinoterb)、DNOC、石肖草酌 (etinofen)及地樂 施(medinoterb); C.13植物生長素除草劑,例如,稗草胺(〇1〇1!16口1'(^)、2,4-D、2,4,5-T、2 甲 4 氯(MCPA>、2 曱 4 氯乙硫酯(MCPA thioethyl)、2,4_滴丙酸(dichlorprop)、精 2,4-滴丙酸 (dichlorprop-P)、2 曱 4 氣丙酸(mecoprop)、精 2 曱 4 氣 丙酸(mecoprop-P)、2,4-E>B、MCPB、草滅平 (chloramben)、麥草畏(dicamba)、2,3,6-TBA、殺草 143575.doc -60- 201018400 畏(tricamba)、二氣啥嚇酸(quinclorac)、氯甲噎琳酸 (quinmerac)、二氣 °比 π定酸(clopyralid)、氟草煙 (fluroxypyr)、毒莠定(picloram)、三氯比(triclopyr) 及草除靈(benazoline); C. 14植物生長素轉運抑制劑,例如,萘草胺(naptalam)及 二 I D比隆(diflufenzopyr); C· 15新燕靈(Benzoylprop)、麥草氟(flamprop)、麥草氟甲 S旨(flamprop-M)、漠 丁草胺(bromobutide)、整形醇 (chlorflurenol)、環庚草鍵(cinmethylin)、甲基殺草 隆(methyldymron)、乙氧苯草胺(etobenzanid)、殺木 膦(fosamine)、美坦(metam)、稗草丹(pyributicarb)、 去稗安(oxaziclomefone)、邁隆(dazomet)、三氟草胺 (triaziflam)及漠甲烧(methylbromide)。 適宜安全劑可選自以下列示:解草酮(benoxacor)、解毒 喧(cloquintocet)、解草胺腈(cyometrinil)、二氣丙烯胺 (dichlormid)、二環酮(dicyclonon)、二乙基苯基硫代鱗酸 醋(dietholate)、解草0坐(fenchlorazole)、解草咬(fenclorim) 、解草胺(flurazole)、將草安(fluxofenim)、解草°惡0坐 (furilazole)、雙苯°惡°坐酸(isoxadifen)、°比唾解草醋 (mefenpyr)、 美芬尼特(mephenate)、環烧酸肝 (naphthalenic anhydride)、2,2,5-三甲基-3-(二氯乙醯基)-1,3-噁唑啶(R-29148)、4-(二氯乙醯基)-1-氧雜_4_氮雜螺 [4.5]癸烷(AD-67 ; MON 4660)及解草腈(oxabetrinil)。 生長調控劑之實例係1-萘基乙醯胺、1-萘基乙酸、2-萘 143575.doc -61 - 201018400 基氧基乙酸、3-CPA、4-CPA、°密咬醇(ancymidole)、蒽酉昆 (anthraquinone)、BAP、三丁鱗(butifos〕、脫葉構 (tribufos)、比達寧、整形醇、克美素(chlorm equat)、苯達 〇秦卸(clofencet)、環丙酸醯胺(cyclanilide)、比久 (daminozide)、麥草畏、敵草克(dikegulac-sodium)、α塞節 因(dimethipin)、殺蜗醇(chlorfenethol)、乙稀基石夕烧 (etacelasil)、乙烯利(ethephon)、0引熟醋(ethyehlozate)、 2,4,5-洋丙酸(fenoprop)、2,4,5-TP、增糖胺(fluoridamid)、 吱嘴醇(flurprimidol)、護汰芬、赤徽酸(gibbezrellic acid)、 赤徽素(gibberellin)、雙胍辛胺、0弓丨°朵丁酸、0弓丨0朵乙酸、 卡若他贊(karetazan)、凯因庭(kinetin)、1-(乙氧基幾基)-乙基-3,6-二氣-2-甲氧基苯甲酸乙醋(lactidiehlor-ethyl)、 馬來酿肼(maleic hydrazide)、說績醯草胺(mefluidide)、縮 節胺(mepiquat-chloride)、萘草胺、巴克素(pa_clobutrazole) 、調環酸妈鹽(prohexadione-calcium)、氯曱嗜淋酸 (quinmerac)、殺雄淋(sintofen)、調節稀(tetcyclacis)、°塞 苯隆、三块苯甲酸、抑芽°坐(triapenthenol)、三載燦 (triazethan)、脫葉磷、抗倒醋(trinexapac-ethyl)及稀效0坐 (uniconazole) ° 就種子處理而言,植物保護劑較佳選自具有殺真菌、殺 昆蟲、殺蟎及/或殺線蟲活性之有機物質。持定言之,其 為以下物質中之一或多種: 具有殺真菌活性之物質,例如群組A. 1之殼真菌劑,特 定言之唑史卓賓、克收欣、歐沙史卓賓、派拉克史卓賓或 143575.doc -62- 201018400
二氟敏;群組A.2之殺真菌劑,特定言之二曱馬夫、萎鏽 靈、矽硫芬以及N-二苯基醯胺,例如波斯卡利 '必殺酚或 N-(3|,4|,5|_三氟聯苯_2_基)_3_二氟甲基甲基吡唑_4_曱醯 胺;群組Α·3之殺真菌劑,特定言之免賴得、多菌靈、惡 黴靈、依滅列、撲克拉、腐絕、以及三唑類,例如,地芬 康唑、環氧康唑、氟喹康唑、護汰芬、麥康唑、撲硫康 唑、得克利、三泰隆或三替康唑、以及滅達樂、右滅達樂 (精甲霜靈)、歐殺斯、雙胍辛胺、比利美沙尼、鏈黴素、 依普同、氟二惡尼或蓋普丹。 具有殺昆蟲或殺蟎或殺線蟲活性之物質,例如啶蟲脒、 &赛滅寧、β-赛滅寧、聯苯菊酯、蟲蟎威、丁硫克百威、 可尼丁、乙氛菊醋、賽扶寧、赛滅寧、漠氰菊_、二氣苯 隆、達特南、依芬普司、苯丁錫、甲氰菊酯、費普尼、護 赛寧、吡蟲啉、λ-赛洛寧、尼藤吡藍、信息素類、賜諾 殺、得福隆、七氟菊酯、特丁磷、噻蟲啉、賽速安、硫雙 威、四溴菊酯、唑蚜威、赛滅寧、螺蟲乙酯、氟定菌 鱗、NC 512、唾蟲酿胺、氟蟲酿胺、雙三氟蟲腺、本氣 嗟、DPX-E2Y45、HGW86、比氟普魯、比 f 魯、F_7663、 F-2704、醯胺氟米特、氟酚瑞姆或丁氟蟎酯。 上述植物保護劑可單獨或彼此組合使用。 在本發明之-較佳實施例中,該至少—種植物保護劑〇 具有至多120°C、較佳至多或小於100°C之熔點。 在另一較佳實施例中,本發明調配物包含至少一種植物 保護劑a),根據一尤佳實施例,其為選自以下之殺真菌 143575.doc -63 - 201018400 劑·撲克拉、波斯卡利、派拉克史卓賓、三替康唑、比利 美沙尼、氟喧康唾及N_(3,,4,,5,-三氟聯苯-2-基)-3-二氟曱 基-1-甲基吡唑-4·甲醯胺。 在一尤佳實施例中,本發明調配物含有至少一種群組 A1 ·之殺真菌劑,例如選自以下之活性化合物:唑史卓 賓、二莫西史卓賓、烯肟菌酯、氟咢史卓賓、克收欣、麥 脫明諾史卓賓、比可西史卓賓、派拉克史卓賓、三氟敏、 歐沙史卓賓、(2-氣-5-[l-(3-甲基苄基氧基亞胺基)乙基]苄 基)胺基甲酸曱酯、(2-氣-5-[l-(6-曱基吡啶-2-基曱氧基亞 胺基)乙基]苄基)胺基甲酸甲酯及2-(鄰-(2,5-二甲基苯基氧 基亞甲基)苯基)-3-曱氧基丙烯酸曱酯,尤其為派拉克史卓 賓。 在另一尤佳實施例中,本發明調配物含有至少一種群組 A3.之殺真減劑’特定言之至少一種三α坐或味。坐,例如選 自以下之活性化合物:白特丹羅、溴克嗤、環克嗤、地芬 康唑、烯唑醇、安尼康唑、環氧康唑、芬布康唑、護石夕 得、氟喹康唑、護汰芬、六康嗤、醯胺峻、種菌唾、麥康 唑、麥環丁尼 '潘康唑、普克利、撲硫康唑、矽氟唑、得 克利、四飢利、三泰隆、三泰芬、三替康唾、赛唾法米、 依滅列、稻瘟酯、撲克拉及三氟咪唑。 在又一同樣尤佳之實施例中,本發明調配物含有至少一 種群組Α1.之殺真菌劑’其較佳選自唑史卓賓、二莫西史 卓賓、烯肟菌酯、氟咢史卓賓、克收欣、麥脫明諾史卓 賓、比可西史卓賓、派拉克史卓賓、三氟敏、歐沙史卓 143575.doc • 64 - 201018400 2 (2氯-5-[i_(3_f基节基氧基亞胺基)乙基作基)胺基〒
Μ曰、(2-氯-5-Π-(6-甲基吼咬_2_基甲氧基亞胺基)乙基] :基)胺基f酸甲醋及2•(鄰_(2,5_二?基苯基氧基亞尹基) 本基)-3-甲氧基丙烯酸子醋,且其較佳為派拉克史卓賓; 及至少另-種群組A3.之殺真菌齊卜特定言之至少一種三 唑或味唾,例如選自以下之活性化合物:白特丹羅、漠克 唑、環克唾、地芬康嗤、烯唾醇、安尼康唾、環氧康嗤、 芬布康唾、護砂得 '氟喧康唾、護汰芬、六康嗤、酿胺 唑、種菌唑、麥康唑、麥環丁尼、潘康唑、普克利、撲硫 康嗤、石夕氧唾、得克利、四飢利 '三泰隆、三泰芬、三替 康°坐、賽錢米、依滅列、稻㈣、撲克拉及三㈣唾, 尤其為三替康唑或撲克拉或三替康唑與撲克拉之混合物。 本發明調配物通常以調配物總重量之〇丨重量%至4〇重量 %、通常1重量%至30重量%、尤其2重量%至25重量%或5 重量%至20重量%之濃度含有該至少一種植物保護劑。在 多於-種植物保護劑a)之情形下’植物保護劑之總濃度通 常為調配物總重量之〇」重量%至4〇重量%、通常丄重量%至 〇重量/〇尤其2重量%至25重量。/。或5重量。至2〇重量%。 而且’本發明調配物包含水。就未經稀釋調配物之總重 量而言,水的量通常在^至⑽重量。/〇範圍内,通常在 5重量。/〇至50重量%範圍内,尤其在1〇重量%至4〇重量%範 圍内’且較佳在15重量%至3〇重量%範圍内。顯然,水的 量及其他成份的量總計1 〇〇重量%。 在本發明之一較佳實施例中,水性調配物包含: 143575.doc •65· 201018400 a. b. c. d· f. g· 0.1重量%至40重量%、通常1重量%至30重量%、尤其2 重量%至25重量%或5重量%至2()重量%之至少_種如上 所述紙下之水溶解度小於5 g/1之有機植物保護劑, 尤其至少一種較佳或尤佳之植物保護劑; 1重量%至60重量%、通常10重量%至40重量%、尤其15 重量%至35重量。/。之至少_種如上所述溶劑…,尤其至 少一種描述為較佳或尤佳之溶劑b); 1重量/〇至60重置%、通常1〇重量%至4〇重量%、尤其Η 重量%至35重1 %之至少—種如上所述溶劑y,尤其至 少一種描述為較佳或尤佳之溶劑c); 1重量%至60重量%、通常5重量%至45重量%、尤其1〇 重量/。至35重量%之至少一種如上所述溶劑d广尤其至 少一種描述為較佳或尤佳之溶劑d); 0.5重量%至30重量%、通常2重量%至25重量%或4重量 %至24重量%、尤其5重量%至2〇重量%之至少一種如上 所述非離子型表面活性劑e),尤其至少—種描述為較 佳或尤佳之表面活性劑e); 0.5重量❶/◦至25重量%、通常i重量%至25重量%或i重量 %至20重量❶/❶、尤其5重量%至15重量%之至少一種如上 所述陰離子型表面活性劑f),尤其至少一種描述為較 佳或尤佳之表面活性劑f);及 水補足至1 00重量。/Q,例如佔1重量%至80重量。/❶,通 韦在5重量%至5〇重量%範圍内,尤其在1〇重量%至4〇 重量%範圍内且更尤其在15重量%至3〇重量%範圍内。
143575.doc -66- 201018400 對於組份a)-f)之重直比’尤其對於表面活性劑e)+f)之總 量、溶劑b)+c)+d)之總量、表面活性劑e)+f)加上溶劑 b)+c)+d)之總量、表面活性劑e)+f)之總量與植物保護劑a) 之比、表面活性劑e)+f)之總量與溶劑b)+c)+d)之總量的比 及表面活性劑e)+f)加上溶劑b)+c)+d)之總量與植物保護劑 a)之比,上文所述亦適用。 而且,本發明調配物可包含常用佐劑,例如,防泡劑 (消泡劑)、防腐劑(殺細菌劑)、著色劑、穩定劑、增桐 劑、黏著劑、防凍劑及常用於水性殺蟲劑調配物中之其他 物質。該等佐劑之總量通常佔未經稀釋調配物重量之不大 於20重量%、尤其不大於15重量%。除防凍劑及著色劑 外,各佐劑的量通常不超過5重量%,且尤其不超過3重量 %。 適宜防泡劑包含聚石夕氧烧,例如,聚二甲基石夕氧烧、長 鏈醇、有機氟化合物、脂肪酸及其鹽、及該等之混合物。 防泡劑通常以每升調配物0.1克至5克的量使用。 用於防止本發明組合物受細菌感染之適宜防腐劑包含曱 酸、對羥基苯曱酸之烷基酯、苯甲酸鈉、2-溴-2-硝基丙 烧-1,3-二醇、鄰·笨基龄、雙氯齡、苯曱醇半縮甲路、嚷 °坐啉酮及異噻唑啉酮衍生物,例如,烷基異噻唑啉酮及苯 并異噻唾啉酮、5-氣-2-曱基-4-異噻唑啉酮、五氯酚、2,4-二氯苯甲醇、及該等之混合物。適宜市售殺細菌產品之實 例係 Proxel® (ICI)、Acticide® RS (Thor Chemie)、Kathon® (Rohm & Haas)及Acticide MBS (Thor Chemie)。通常,防 143575.doc -67- 201018400 腐劑的量為每升調配物0·1克至10克。 著色劑之實例係微溶於水之顏料及溶於水之染料二者。 可提及之實例係名為下列之染料·羅丹明B (Rh〇damin 、C.1.顏料'红及C.I·溶劑紅1、及顏料藍15 j、顏料藍 15.3顏料藍丨5:2、顏料藍15:1、顏料藍8〇、顏料黃1、顏 料黃13、顏钋紅U2、顏料紅48:2、顏料紅48:1、顏料紅 5 7.1顏料紅53:1、顏料撥43、顏料燈34、顏料橙f、顏料 綠36、顏料絲7、顏料白6、顏料棕25、鹼性紫⑺、鹼性紫 49、酸性紅5L、酸性紅52、酸性紅14、酸性藍9、酸性黃 23、鹼性紅1〇、鹼性紅1〇8、酸性紅18、食品紅1、食品紅 2及食品紅7。 適宜穩定Μ包含(例如)UV吸收劑,例如,肉桂酸酯、 3,3-二苯基-2-氰基丙烯酸酯、經羥基及/或烷氧基取代之二 本甲酮、N-(瘦基本基)_苯并三唾、經基笨基s三唤草 醯胺及水楊酸酯’例如UVINUL® 3000、3008、3040、 3048、3049、3050、3030、3035、3039、3088、UVINUL® MC80 ’及自由基清除劑’例如,抗壞血酸、檸檬酸、空 間位阻胺(稱為HALS化合物)’例如,UVINUL® 4049H、 4050H、5050H及諸如此類;及抗氧化劑,例如維生素e。 在一較佳實施例中,穩定劑係檸檬酸或抗壞血酸。通常, 穩定劑的量在每升調配物0.01克至1〇克範圍内。 增稠劑(即可改變調配物之流動性質之化合物,即靜止 時南黏度且挽動態時低黏度)之實例係多糖,例如黃原膠 (Kelzan®, Ke lco) ^ Rhodopol® 23 (Rhone Poulenc) ic 143575.doc -68· 201018400
Veegum® (R.T. Vanderbilt)及諸如 Attaclay® (Engelhardt)等 有機及無機層狀礦物質。 黏著劑或膠黏劑之實例係環氧乙烷或環氧丙烷嵌段聚合 物表面活性劑以及聚乙烯醇、聚乙酸乙烯酯、部分水解之 聚乙酸乙烯酯、聚乙烯基吡咯啶酮、聚丙烯酸酯、聚曱基 丙烯酸酯、聚丁烯、聚異丁烯、聚苯乙烯、聚乙烯胺、聚 乙稀酿胺、聚乙稀亞胺(Lupasol®、Polymin®)、聚醚及衍 生自上述聚合物之共聚物。 ❹ 適宜防;東劑之實例係(Cl_C4)_烷醇,例如乙醇、異丙 醇、正丁醇、異丁醇;以及(c2_C6)_多元醇,例如甘油、 乙二醇、己二醇及丙二醇;及該等之混合物。 該等常用添加劑可早已在本發明組合物製備期間添加, 或另一選擇為在用水稀釋以製備即用組合物時或之後才添 加。 通常,本發明調配物可藉由將各成份簡單混合直至形成 φ 外觀均質之流體來製備。各成份之添加順序通常不甚重 要。例如,可將各成份放置於容器中,並 由此獲得之混合物均質化,直至形成均質液體。然= 可百先將有貞植物保護劑與至少一種表面活性劑e)溶解於 /合劑b)、c)及/或句中之至少一者或該等溶劑之混合物中, 並藉由例如將該溶液添加至水中或藉由將水添加至該溶液 中使所得/合液與水及其他成份混合。混合期間之溫度及其 他混合條件不甚重要。通常,成份之混合係在HTC至 尤其10C至60C之溫度下實施。諸如351或4〇。〇或 143575.doc •69· 201018400 更高等較高溫度可能有利於加速調配物之形成。另一方 面,混合通常亦可在較低溫度(約1 〇°C至3 5 )下實施。 端視所用植物保護劑之性質而定,本發明調配物可用於 控制許多種有害物,且可用於處理植物農作物及種子及無 生命物質及用於家用目的。 在本文中,「有害物」或「有害生物體」應理解為意指 可使用有機植物保護劑(即殺蟲劑,尤其殺真菌劑及殺真 菌劑與其他殺蟲劑之混合物)防治或控制之所有有害物類 型。因此術語有害物包含植物致病(即有害)生物體,尤其 有害真菌及其孢子;以及有害昆蟲、物蛛類動物、線蟲及 有害植物。術語「控制」包括治癒性處理,即用本發明調 配物處理受侵染之植物;以及保護性處理,即對植物進行 處理以保護其免於被有害物侵染。 因此,本發明亦係關於: -本文所述調配物用於控制有害物、特定言之植物致病 有害物之用途;及 -控制有害生物體、特定言之植物致病生物體之方法, 其包含使有害生物體、其棲息地、其宿主(例如植物及 種子)及土壤、其生長或可能生長之區域及環境、以及 擬實施保護以免於被植物致病生物體侵襲或感染之物 質、植物、種子、土壤、表面或空間與有效量之本發 明調配物接觸。 本發明之另一態樣係關於本文所述調配物用於保護植物 (包括種子)、尤其用於保護有用植物免於被有害生物體侵 M3575.doc 201018400 襲之用途。因此,本發明亦係關於該等調配物用於控制植 物致病生物體(例如,有害真菌、昆蟲、蜘蛛類動物、線 蟲及有害植物)之用途。根據一較佳實施例,本發明係關 於該等調配物用於保護種子免於被有害真菌、昆蟲、蜘蛛 類動物及線蟲侵襲、尤其免於被有害真菌侵襲之用途。 本發明調配物可以未經稀釋形式或水稀釋物形式施用。 根據一較佳實施例,該等調配物係以未經稀釋形式使用。 ❷ 在另一較佳實施例中,在施用之前,將調配物用至多50份 水、較佳至多10份水且尤佳至多3份水/每份調配物進行稀 釋,所有份數皆意指重量份數。 稀釋通常藉由將本發明調配物傾倒至水中來達成。通 常,利用攪動(例如,攪拌)來使濃縮物與水快速混合。然 而,通常並不需要攪動。儘管溫度對於稀釋過程而言並非 重要因素,但稀釋通常在〇t至5(rc、尤其1〇t至3〇它之 溫度下或在環境溫度下實施。 φ 用於稀釋之水通常為自來水。然而,該水可早已包含用 於植物保護之水溶性化合物,例如營養素、肥料或殺蟲 劑。 本發明調配物(視情況呈稀釋形式)係利用熟習此項技術 者所習知之方法及裝置來使用或施用。特定言之,可藉由 常用種子處理技術使用其來處理種子,例如藉由摔種、種 ^塗敷、種子浸泡、種子膜塗敷、種子多層塗敷、種子包 殼、種子濕透、種子撒粉及種子粒化。 根據種子處理之第-實_,用本發”配物或其水性 143575.doc -71· 201018400 稀釋物對種子(即能夠繁殖且擬用於播種之植物部分)進行 處理。在本文令,術語種子包含種子及能夠繁殖之任一類 型植物部分,包括種子、種子榖粒、種子部分、suckle、 果實、塊莖、穀物穀粒、插條或諸如此類,尤其為縠粒及 種子。 種子處理可藉由例如將種子與本發明植物保護調配物或 與藉由在播種之前及植物出苗之前用水稀釋自此獲得之喷 射混合物混合、用其喷射種子或使種子被霧籠罩(fog)而達 成。該等措施可在用於種子處理之特定裝置(例如條播機 (seed drill))中實施。然而,該處理亦可簡單地藉由將本發 明水性調配物與種子混合於容器(例如桶或盤)中並隨後乾 燥種子來實施。 或者’種子亦可在播種期間用本發明植物保護調配物進 行處理。 在本發明種子處理或土壤處理之又一實施例中,將本發 明調配物引入已經包含種子之犁溝中。或者’亦可首先用 本發明調配物處理種子犁溝並隨後將種子引入種子犁溝 中。 在本發明又一實施例中,用該等調配物對所生長之植物 進行處理(尤其藉由喷射)。為此’可將呈未經稀釋形式或 呈水性稀釋物形式之調配物施用至植物。 通常,本發明調配物之施用方式應端視擬定目的而定; 在任何情況下,應確保存在於調配物中之植物保護劑的分 佈盡可能地細密。 143575.doc • 72· 201018400 所選用於種子處理之本發明調配物的量應能夠使種子與 有效量之存在於調配物中之植物保護劑接觸。通常,每 100 kg種子使用包含〇1吕至1〇 kg、尤其J吕至5 kg且尤其1 g至2.5 k g植物保護劑或該等活性物質之混合物的量之本發 明調配物。對於某些有用植物(例如,萵苣及洋蔥),擬用 活性物質的量可能較大》 端視所用活性物質之性質而定,本發明調配物適於處理 φ 任一有用植物之種子,例如榖類農作物、塊根農作物、油 料農作物、蔬菜、香料作物、供裝飾用之植物及諸如此 類,例如用於處理以下植物之種子:硬質小麥及其他小麥 物種、热麥、黑麥、大麥、玉米(包括飼用玉米及甜玉 米)大豆、云苔、棉花、向日葵、香蕉、水稻、油菜、 甜菜、糖用甜菜、飼用甜菜、茄子、馬鈐薯、草皮、草種 子西、’工柿韭慧、南瓜(pumpkin/squash)、捲心菜、萬 望、鈴狀椒、黃瓜、甜瓜、豆類、婉豆、大蒜、洋慧、胡 φ 蘿蔔、煙草、葡萄、矮牵牛花、天竺葵、老鸛草、三色堇 及諸如此類。 本發明調配物亦適於處理因基於育種、突變及/或遺傳 工程之方法而對除草劑、殺真菌劑、殺昆蟲劑或殺線蟲劑 具有抗性之有用植物的種子。例如,調配物可用於處理對 選自由下列組成之群之除草劑具有抗性之轉基因植物之種 子.石買醯脲(EP A 0 257 993、美國專利第5,013,659號)、 咪唑啉酮(參見例如美國專利第6,222,1〇〇號、W〇 01/82685、WO 00/26390、WO 97/41218、WO 98/02526、 143575.doc -73- 201018400 WO 98/02527、WO 04/106529、WO 05/20673、WO 03/14357、WO 03/13225、WO 03/14356、WO 04/16073)、 草銨膦及相關化合物(參見例如EP-A-0 242 236、EP-A-242 246)及草甘膦及相關化合物(參見例如WO 92/00377),或 用於處理對選自環己二烯酮/芳氧基苯氧基丙酸除草劑(美 國專利第5,162,602號、美國專利第5,290,696號、美國專利 第5,498,544號、美國專利第5,428,001號、美國專利第 6,069,298號、美國專利第6,268,550號、美國專利第 6,146,867號、美國專利第6,222,099號、美國專利第 6,414,222號)群組之除草劑具有抗性之植物的種子,或用 於處理轉基因有用植物(例如,棉花及玉米)之種子,轉基 因有用植物能夠產生蘇雲金芽孢桿菌(Bacillus thuringiensis) 毒素(Bt毒素),此賦予對某些有害物之抗性(EP A 0 142 924、EP A 0 193 259)。 而且,本發明調配物可用於處理特性經改良而優於現有 植物且可例如藉助傳統育種方法及/或突變或藉由重組方 法產生之植物的種子。因此,農作物植物之重組變體之產 生已多次闡述,其目的係改良該等植物之澱粉(例如WO 92/1 1376、WO 92/14827、WO 91/19806)或改良該等植物 之脂肪酸組成(WO 91/13972)。 按照本發明處理之種子因與傳統處理種子相比具有有利 特性而與眾不同,且因此亦為本申請案之標的物。 以下實例意欲闡釋本發明。 I.調配物之製備(通用方案) 143575.doc -74- 201018400 使用表1中所詳述之組份。 表1 :表2中所列示調配物之組份a)至f)的例子。 a) b)* C)* d)** e) f) 撲克拉 γ-丁内酯 (可混溶) 苯乙酮 (5.5 g/l) Agnique® KE 3658 Lutensol® T05 Lutensit® A-BO 派拉克史 卓賓 Arcosolv® PMA (1-甲氧基-2·丙醇 乙酸酯) (400 g/1) Agrisol PX401 (24 g/l) Edenor® Ή 05 Lutensol® T07 Soprophor® DSS 15 三替康唆 己二醇 (500 g/l) 苯甲醇 (39 g/l) Solvesso@ 150 ND Lutensol ⑧ T015 Soprophor® 4D384 Purasolv® NPL (乳酸正丙基酯) (可混溶) 碳酸丁二 酯 Solvesso® 200 ND Lutensol® XP50 DMSO (可混溶) 甘油三乙 酸酯 (64 g/l) 十二烷醇 Lutensol® XP140 四氫糠醇(可混溶;) 環己酮 (24 g/l) Rhodiasolv® DIB Pluronic PE 6400 2-庚酮 (4.3 g/n 乳酸2-乙基己 基酯 S-MAZ® 20 Soprophor® S25 T-MAZ® 20
*各溶劑在20°c下於水中之溶解度在括號中給出。可混 溶意指可與水完全混溶。 "群組d)之所有溶劑在2〇°c下具有小於0.1 g/ι之水溶解 度。 組份a)至f)對應於本發明調配物之組份約至〇。 商標名之說明: 143575.doc -75- 201018400
Edenor® ΤΙ 05 :高油酸含量之脂肪酸混合物(c〇gnis); Agnique® KE 3658 :脂肪酸二甲基醯胺(Cognis);
Agrisol PX401 : 2-苯氧基乙醇(Akzo Nobel);
So丨vesso® 150 ND :主要為C!。-烧基苯及Ch-烧基苯,沸點 介於175°C至209°C範圍内,萘已脫去(ExxonMobil
Chemical);
Solvesso® 200 ND :主要為C10-烧基萘及(:14-烧基萘,沸點 介於235 C至305 C範圍内,萘已脫去(ExxonMobil
Chemical); 1^6118〇丨@1'05:具有5個環氧乙烷(£0)單元之(:13-羰基合 成醇聚乙氧基化物,HLB值:10.5 (BASF);
Lutensol® T07 :具有7個EO單元之C13-羰基合成醇聚乙氧 化物,HLB 值為 12.0 (BASF);
Lutensol® T015 :具有15個EO單元之C13-羰基合成醇聚乙 氧化物,HLB值為15.5 (BASF);
Lutensol® XP50:具有5個EO單元之2-丙基庚醇聚乙氧基 化物,HLB值:11.5 (BASF);
Lutensol® XP140:具有14個EO單元之2-丙基庚醇聚乙氧 基化物,HLB值:16.0 (BASF);
Soprophor® S 25:具有乃個EO單元之三苯乙烯基酚聚乙 氧基化物,HLB值:14_5 (Rhodia); S-MAZ® 20:山梨糖醇酐單脂肪酸酯(主要為單十二烷酸 酯),HLB值:8.0 (BASF); T-MAZ® 20 :具有約20個EO單元之聚乙氧基化之山梨糖醇 143575.doc -76 - 201018400 酐單月桂酸酯,HLB值:16.7 (BASF);
Pluronic PE 6400 :環氧丙烷/環氧乙烷嵌段聚合物,EO含 量約為 40% (BASF);
Lutensit® A-BO : 2-磺醯基二辛基琥珀酸鈉(BASF); Soprophor® DSS 15:具有15個EO單元之乙氧基化之二苯 乙烯基盼硫酸鹽(Rhodia)
Soprophor® 4D 384:具有16個EO單元之乙氧基化之三苯 乙稀基盼硫酸銨(Rhodia)。
Rhodiasolv® DIB :戊二酸二異丁基酯、琥珀酸二異丁基 酯及己二酸二異丁基酯之混合物(Rhodia)。 本發明之調配物1至26列示於表2中。表2亦顯示用於製 備各調配物之組份及其量。該製備係如下文所述實施,所 有步驟皆在室溫(RT)下實施: 將一或多種組份A之組份放置於容器中,且在添加三種 或更多種組份B、C及D後,攪拌混合物,直至A盡可能完 全地溶解。此後,邊小心攪拌邊添加兩種或更多種組份E 及F,且持續攪拌,直至獲得盡可能均質之溶液。此後, 邊攪拌邊添加蒸餾水,並攪拌混合物,直至獲得澄清調配 物。 II. 本發明調配物之穩定性測試 將所製備調配物在RT下靜置過夜,並隨後宏觀測定其 外觀。均質且澄清流體表明微乳液保持穩定,而朦朧或乳 狀外觀則表明微滴尺寸顯著增大且微乳液可能轉化成普通 乳液。 143575.doc -77- 201018400 隨後’將各調配物在-10°c或54°c下儲存3天,並隨後如 上所述實施宏觀檢測°再次,澄清均質外觀表 明微乳液在 該等條件下穩定。將形成紋影(schHeren)視為調配物在給 定條件下儲存較長時間可能導致相分離之可能性的跡象。 調配物束結表明冰點相對較高,其可藉由例如添加防凍劑 來降低。 結果匯總於表2中。 表2 :調配物之製備及穩定性 序號 1 2 3 4 5 6 7 8 9 10 11 12 派拉克史卓賓 10.0 g 10.0 g 10.0 g 10.0 g 10.0 g 撲克拉 5.0 g 5.0 g 5.0 g 15.0 g 15.0 g 10.0 g 15.0 g DMSO 2.5 g 2-5 g 2.5 g 2.5 g 2.5 g Arcosolv PMA 20.0 g 20.0 g 20.0 g 20.0 g 己二醇 10.0 g 10.0 g 15.0 g 15-0 g 15.0g 15.0 g 15.0 g Purasolv NPL 20.0 g 苯乙酮 20.0 g 20.0 g 15.0 g 笨曱醇 17.5 g n.5g 17.5 g 17.5 g 17.5 g 碳酸丁二酯 環己酮 20.0 g 15.0 g 17.5 g 17.5 g Agnique KE 3658 10.0 g 10.0 g 10.0 g 10.0 g Edenor ΤΙ 05 10.0 g Solvesso 150ND 17.5 g n.5g 17.5 g 17.5 g 17.5 g 17.5 g 17.5 g Lutensit A-BO 5.4 g 5.4 g Lutensol TO 5 3.6 g Lutensol TO 7 7.2 g 7.2 g 7.2 g 7.2 g 7.2 g Lutensol TO 15 3.6 g Lutensol XP 50 3.6 g 143575.doc -78- 201018400 序號 1 2 3 4 5 6 7 8 9 10 11 12 Lutensol XP 140 3.6 g Pluronic PE 6400 7.2 g S-Maz20 Soprophor 4D384 7-2 g 7.2 g 7.2 g 7.2 g 7.2 g 10.8 g 10.8 g 10.8 g 10.8 g 10.8 g Soprophor S 25 3.6 g 3.6 g 3.6 g 3.6 g 3.6 g 12.6 g 12.6 g 7-2 g T-Maz20 7.2 g 水 24.5 g 24.5 g 24.5 g 19.5 g 19.5 g 27.0 g 22.0 g 22.0 g 22.0 g 22.0 g 22.0 g 22.0 g 1 d後之穩定性 澄清 澄清 澄清 澄清 澄清 燈清 澄清 澄清 澄清 澄清 澄清 澄清 -lOt,3d 澄清 澄清 澄清 澄清 澄清 澄清 澄清 澄清 澄清 澄清 澄清 澄清 +54〇C * 3d 有紋影 澄清 潑清 澄清 潜清 澄清 澄清 澄清 澄清 澄清 澄清 澄清
表2(續) 序號 13 14 15 16 17 18 19 20 21 22 23 派拉克史卓賓 10.0 g 10.0 g 10.0 g 10.0 g 10.0 g 10.0 g 2.0 g 2.0 g 2.0 g 2.0 g 2.0 g 撲克拉 6.9 g 6.9 g 6.9 g 6.9 g 6.9 g 三替康唑 1.5 g 1.5 g 1.5 g 1.5 g 1.5 g DMSO 2.5 g 2.5 g 2.5 g 2.5 g 2.5 g 己二醇 15.0 g 15.0 g 15.0g 15.0 g 15.0 g 15.0 g 20.0 g 20.0 g 20.0 g 20.0 g PuTasolv NPL 20.0 g 苯乙酮 17.5 g 17.5 g 17.5 g Agrisol PX 401 15.0 g 15.0 g 苯曱醇 17.5 g 17.5 g 17.5 g 碳酸丁二酯 15.0 g 甘油三乙酸酯 15.0 g 15.0 g Agnique KE 3658 10.0 g 10.0 g 10.0 g 10.0 g 1-十二烷酵 10.0 g Solvesso 150ND 17.5 g 17.5 g 17.5 g Solvesso 200 ND 17.5 g 17.5 g 17.5 g Lutensit A-BO 7-2 g 7-2 g -79- 143575.doc 201018400 序號 13 14 15 16 17 18 19 20 21 22 23 Lutensol TO 5 3.6 g 3.6 g Lutensol TO 7 7.2 g 7.2 g 7.2 g V-2g 7.2 g Lutensol TO 15 10.8 g 3.6 g Lutensol XP 50 3.6 g Lutensol XP 140 3.6 g Pluronic PE 6400 S-Maz 20 7.2 g Soprophor 4D384 10.8 g 10.8 g 7-2 g 7.2 g 7.2 g 7.2 g 7.2 g Soprophor DSS 15 10.8 g 10.8 g Soprophor S 25 3.6 g 10.8 g 3.6 g 3.6 g 3.6 g 3.6 g 3.6 g T-Maz 20 水 22.0 g 22.0 g 22.0 g 22.0 g 22.0 g 22.0 g 24.1 g 24.1 g 24.1 g 24.1 g 24.1 g 1 d後之穩定性 澄清 澄清 澄清 澄清 澄清 澄清 澄清 澄清 澄清 澄清 澄清 -10°C > 3d 澄清 澄清 澄清 澄清 澄清 澄清 澄清 澄清 )東結 澄清 澄清 +54°C,3d 澄清 澄清 澄清 澄清 澄清 澄清 澄清 澄清 有一些 紋影 澄清 澄清 表2 (續) 序號 24 25 26 VI V2 派拉克史卓賓 12.0 g 12.0 g 12.0 g 撲克拉 44.1 g 44.1 g 44.1 g 5.0 g 15.0 g 三替康唑 16.0 g 16.0 g 16.0 g DMSO 25,0 g 25.0 g 25.0 g 2.5 2.5 己二醇 200 g Plurasolv NPL 20.0 g 四氫糠醇 200 g 200 g 苯乙酮 20.0 g 碳酸丁二酯 150 g 甘油三乙酸酯 150 g 150 g 10.0 g -80- 143575.doc 201018400 參 序號 24 25 26 VI V2 Agnique KE 3658 10.0 g Edenor ΤΙ 05 100 g 32.5 g Rodiasolv DIB 100 g 乳酸2-乙基己基酯 100 g Lutensit A-BO Lutensol TO 5 80 g 80 g 80 g 4.0 g Lutensol TO 7 18.0 g Soprophor 4D384 80 g 80 g 80 g SoprophorDSS 15 10 g 10 g lOg Soprophor S 25 16.0 g 紅染料1 40 g 40 g 40 g Bacterizide2 2g 2g 2g 水 260.9 g 260.9 g 260.9 g 24.0 g 20.0 g 1天後之穩定性 澄清 澄清 澄清 乳液 乳液 -l〇t,3d 有一些紋影 有一些紋影 潑清 n.d. n.d. +54〇C > 3d 有紋影 有紋影 有紋影 n.d. n.d. 143575.doc •81- 1 酸性紅1 8 2 甲基異噻唑啉酮與苯并異噻唑啉酮之混合物: • Acticide® MBS,Thor GmbH, Speyer ΠΙ· 拌料種子之檢測 使用以下調配物來實施比較實驗: 調配物V3 : Abavit UF (BASF);其為傳統種子處理調配 物,主要包含活性物質萎鏽靈及撲克拉及有機溶劑N-曱基 吡咯啶酮。V3在下文中以未經稀釋形式使用。 調配物V4 : Kinto Duo (BASF);其為包含撲克拉及三替 康唑之傳統水性種子處理懸浮液。實例24、25及26之調配 201018400 物及市售調配物V4在下文中以稀釋形式使用,其中每份調 配物用1份水稀釋。 A)拌種(通用方案) 拌種係使用藉由上文方案製備之呈拌種漿液形式之調配 物來實施。使用SATEC之拌種機,其中藉由轉子_定子原 理將種子混合’並藉助旋轉盤來噴射拌種漿液。轉子速度 調節至200 rpm,且在壓縮空氣供給之壓力計處將機器之 空氣流動調節至960 Ι/h。所用拌種漿液係按照上文方案製 備之調配物。拌種漿液之期望量係使用軟管幫浦來計量, 軟管末端固定在旋轉盤上方的短距離處。市售拌種調配物 V3及實例調配物19、21及23之施用率各為2 ml/kg。市售 拌種調配物V4及實例24、25及26之調配物(其已以1:1 v/v 比率用水稀釋)各以4 ml/kg施用。若需要,則對擬拌料之 種子進行清洗,且在2(TC&50%大氣濕度之受控環境櫥中 適應24小時以創造更具再現性之條件。在將2 kg種子引入 機器中後,啟動旋轉盤,並藉由啟動幫浦而開始拌種。3〇 秒後’藉由放出種子而結束拌種。 B)流動性之檢測 測定拌料種子流出振動漏斗所花費之時間,且用作流動 I·生之量度。為此,拌種後即刻將所有種子(2 kg)放置於漏 斗中,漏斗流出孔之直徑為2_8 cm且以15瓜出之振幅振 動。利用該方法,將用實例19、21、23、24、25及26之調 配物處理之小麥種子與用市售拌種調配物V3及V4處理之 種子進行比較。在所有情形下皆使用藉由上文方法拌料之 143575.doc 201018400 種子。 由此獲得之流動性質結果匯總於表5中。 表5 :拌料小麥種子之流動性質比較 流動性 (與未經處理種子相比) 未經處理 100% 調配物V3 87% 調配物V4 70% 實例19 91% 實例21 91% 實例23 91% 實例24 80% 實例25 80% 實例26 80% C)粉塵形成之檢測
該等檢測係在上述拌種實施後一天在相同拌種機器中實 施。在此期間,將拌料種子於20°C及50%大氣濕度之受控 環境櫥中儲存24小時。轉子速度及通過機器之空氣流動如 上所述進行設置,且出於適應目的使機器運行10分鐘。藉 由抽吸使預先稱重之渡紙(Fisherbrand玻璃纖維遽紙38 mm,產品號為FB59403)墊入拌種機之蓋子中。此處,真 空幫浦抽取通過機器的加壓空氣的一部分,其包括可能產 生之任何粉塵。隨後,隨著幫浦及轉子運轉,向機器中裝 入1 kg種子,且幫浦在30秒後停止。稱重濾紙,且因此測 定粉塵殘留(以克/100 kg種子計)。 利用該方法,將用實例19、21、23、24、25及26之調配 143575.doc -83 - 201018400 物拌種之小麥穀物與用市售拌種凋配物V3及V4拌種之小 麥穀物進行比較。由此獲得之粉塵形成結果匯總於表6 中 〇 表6 :拌料小麥種子之粉塵形成比李交 粉塵形成[g/l〇〇kg] 未經處理 0.46 調配物V3 0.05 調配物V4 0.86 實例19 0.01 實例21 0.04 實例23 0.03 實例24 0.00 實例25 0.00 實例26 0.00 143575.doc 84-
Claims (1)
- 201018400 七、申請專利範圍: 1. 一種液態水性之植物保護調配物,其包含 a) 至少-種2(TC下之水溶解度小於5g/i的有機植物 保護劑; b) 至^ 一種2〇c下之水溶解度大於1〇〇 ^丨的有機溶 劑; C)至少—種2〇°C下之水溶解度介於2g/l至lOOg/l之 間的有機溶劑; d) 至少一種2〇t下之水溶解度小於2g/1的有機溶 劑; e) 至少一種非離子型表面活性劑; 0至少一種陰離子型表面活性劑;及 g)水。 2·如請求項1之植物保護調配物,其中該至少一種溶劑b)選 自經基化之(C4_C8)·娱:烴叛酸醋、脂族(c2-C8)-二醇及三 醇、(Cs-C8)-烷烴羧酸烷氧基烷基酯、二甲基亞砜、四 氫糠醇、(C3_C4)-碳酸伸烷基酯、ν,Ν·-二曱基-(c3-c4)-伸炫基脲、(C3-C5)-内酯、N-曱基-(c3-c5)-内醯胺及磷酸 二- (Ci-C3)燒基 g旨。 3. 如請求項2之植物保護調配物,其中該至少一種溶劑b)包 含二甲基亞颯。 4. 如請求項3之植物保護調配物,其中該至少一種溶劑b)包 含至少一種除二甲基亞颯以外之第二溶劑b)。 5. 如請求項1至4中任一項之植物保護調配物,其中該至少 143575.doc 201018400 一種溶劑C)選自(c5-c9)-烷烴羧酸烷基酯、(c9-c12)-烷烴 羧酸烷氧基烷基酯、(C5-C9)-二羧酸二烷基酯、(C5-C9)-酮、(C5_C9)-芳基烧基醇、(C5-C9)-芳氧基炫基醇、(c5_ C9)-環烷基醇、(C5_C9)_烷烴二醇烷氧化物、(c5-c9)-烷 烴三醇烷氧化物及(c5-c6)-碳酸伸烷基酯。6. 如請求項1至4中任一項之植物保護調配物,其中該至少 一種溶劑d)選自沸點介於1〇〇。(:至31 〇eC間之脂族、芳香 族及環脂族烴、(C8-C2G)-烷基酚、(C8-C2Q)-烷醇、(Cl〇_ Cm)-炫烴羧酸烷基酯、(C9_C2G)_羥基烷烴羧酸烷基酯、 (Ci2_C28)-環院烴緩酸烧基酿、(c1:2_c28)_環炫(煙二缓酸二 烷基酯、(C丨。二羧酸二烷基酯、烴三醇 烧酸醋、N-(C6-C18)-烷基-(C3-C5)-内醯胺、(c8-c26)-脂 肪酸、其二烷基醯胺及其烷基酯。 7. 如請求項i至4中任一項之植物保護調配物,其中該至少 一種非離子型表面活性劑e)選自多羥基化合杨及具有至少一個寡聚-(CVC4)-伸烷基醚基團之化合物的單脂肪酸 酯。 8·如請求項7之植物保護調配物,其中該至少一種非離 型表面活性劑e)選自山梨糖醇酐單脂肪酸酯、 氧烷之均寡聚物或共寡聚物、寡聚*⑸,氧烷 ⑽院基趟、募聚環氧貌(Ci_Ci6)·烷基苯醚 养聚-(c2-c4)·環敦烧單_、二或三苯乙稀基笨基謎及 聚_(C2-C4)-環氧院單-或二笨乙婦基苯基喊/甲搭縮, 物〇 143575.doc • 2 - 201018400 9·如請求項1至4中任一項之植物保護調配物,其中紅份幻 包含至少兩種具有不同HLB值之非離子型表面活性劑。 10.如請求項9之植物保護調配物,其中組份e)包含至少一種 具有不大於13之HLB值的非離子型表面活性劑及至少一 種具有大於13之HLB值的非離子型表面活性劑。 11·如請求項10之植物保護調配物,其中該具有不大於13之 HLB值的非離子型表面活性劑選自寡聚_(C2_C4)_伸烷基 (C8-C22)-院基喊。 春12·如請求項10之植物保護調配物,其中該具有大於13之 HLB值的非離子型表面活性劑選自環氧丙烷/環氧乙烷嵌 段共寡聚物、寡聚-((VC3)-環氧烷(C8_C22)_烷基醚、寡 聚-(G-C3)-環氧烷單-、二-及三苯乙烯基苯基醚。 13. 如請求項Π之植物保護調配物,其中該具有大於^之 HLB值的轉子型表面活性朗自環氧丙烧/環氧乙燒嵌 段共寡聚物、募聚-(cvc:3)-環氧烷(C8_c22)_烷基醚、募 〇 聚-(C2-C3)_環氧烷單·、二-及三苯乙烯基苯基醚。 14. 如清求項1至4中任一項之植物保護調配物,其包含: a) 0.1重量%至40重量%之至少一種2〇β(:下之水溶解 度小於5 g/Ι的有機植物保護劑; b) 1〇重量%至40重量%之至少—種⑼^下之水溶解度 大於100 g/Ι的溶劑; c) 10重量%至40重量%之至少一種20t下之水溶解度 介於2g/l至l〇〇g/l之間的溶劑; d) 5重量%至45重量%之至少一種2〇r下之水溶解度 143575.doc ·3_ 201018400 小於2 g/l的溶劑; e) 2重量。/。至25重量%之至少一種非離子型表面活性 劑; f) 1重量%至25重量%之至少一種陰離子型表面活性 劑;及 g) 水,補足至1 00重量%。 15 ·如S青求項1至4中任一項之植物保護調配物,其中該至少 一種植物保護劑a)具有至多12(TC之熔點。 16_如凊求項1至4中任一項之植物保護調配物,其中該至少 一種植物保護劑a)係殺真菌劑。 17. 如請求項16之植物保護調配物,其中該殺真菌劑選自唑 類、史卓比尿類(Strobilurins)及雜芳香族羧酸之N_聯苯 基醯胺類群組。 18. 如請求項17之植物保護調配物,其中該殺真菌劑選自撲 克拉(pr〇chl〇raz)、波斯卡利(b〇scalid)、派拉克史卓賓 (pyraclostrobin)、三替康唑(tritic〇naz〇le)、比利美沙尼 (pyrimethanil)、氟喹康唑(fluquinc〇naz〇le)、n_(4,漠聯 苯-2-基)-4-二氟甲基_2_甲基噻唑_5_甲醯胺、N_(4,_三氟 甲基聯苯-2-基)-4-二氟甲基-2-曱基噻唑-5·曱醯胺、N-(4'-氣-31-氟聯苯_2-基)-4-二氟甲基_2-甲基噻唑_5_曱醯 胺、N-(3’,4’-二氯_4_氟聯苯_2_基)_3_二氟甲基曱基〇比 唑-4-曱醯胺及队^^匕三氟聯笨^-基卜夂二氟曱基小 甲基吡唑-4-甲醯胺。 19_如凊求項1至4中任一項之植物保護調配物,其額外包含 143575.doc 201018400 至少一種有機著色劑。 2〇. 一種如請求項1至19中任一項之水性植物保護調配物的 用途’其用於處理植物或種子。 種處理種子之方法’其包含使種子與有效量之如請求 項1至19中任一項之水性植物保護調配物接觸。 22.如明求項21之方法’其中該接觸扣i拊〇·⑶n^ct) 係藉由噴射來達成。 種種子其可藉由如請求項21或22中任一項之方法獲 得。 24. 一種防治植物致病生物體之方法,其包含使該等植物致 病生物體、植物、土壌、該等植物生長或可能生長之區 域或環境與有效量之如請求項1至19中任-項之水性植 物保護調配物接觸。143575.doc 201018400 四、指定代表圖: (一) 本案指定代表圖為:(無) (二) 本代表圖之元件符號簡單說明: Φ 五、本案若有化學式時,請揭示最能顯示發明特徵的化學式: (無)143575.doc
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| UA106213C2 (ru) | 2008-10-10 | 2014-08-11 | Басф Се | Жидкие препараты для защиты растений, содержащие пираклостробин |
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| WO2010052178A1 (de) | 2008-11-07 | 2010-05-14 | Basf Se | Agrochemische formulierung mit drei lösungsmitteln |
-
2009
- 2009-10-08 TW TW098134177A patent/TW201018400A/zh unknown
- 2009-10-09 UY UY0001032169A patent/UY32169A/es unknown
- 2009-10-09 WO PCT/EP2009/063196 patent/WO2010040834A2/de not_active Ceased
- 2009-10-09 AU AU2009301114A patent/AU2009301114B2/en not_active Expired - Fee Related
- 2009-10-09 AR ARP090103909A patent/AR075284A1/es unknown
- 2009-10-09 BR BRPI0919701-0A patent/BRPI0919701A2/pt not_active IP Right Cessation
- 2009-10-09 EA EA201100596A patent/EA021204B1/ru not_active IP Right Cessation
- 2009-10-09 UA UAA201105743A patent/UA106732C2/uk unknown
- 2009-10-09 US US13/122,790 patent/US8716182B2/en not_active Expired - Fee Related
- 2009-10-09 EP EP09783906A patent/EP2348833A2/de not_active Withdrawn
- 2009-10-09 CN CN2009801401849A patent/CN102176821A/zh active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| UA106732C2 (uk) | 2014-10-10 |
| AU2009301114A1 (en) | 2010-04-15 |
| WO2010040834A3 (de) | 2010-12-09 |
| US8716182B2 (en) | 2014-05-06 |
| AR075284A1 (es) | 2011-03-23 |
| BRPI0919701A2 (pt) | 2015-08-18 |
| EP2348833A2 (de) | 2011-08-03 |
| EA201100596A1 (ru) | 2011-12-30 |
| AU2009301114B2 (en) | 2015-03-19 |
| CN102176821A (zh) | 2011-09-07 |
| WO2010040834A2 (de) | 2010-04-15 |
| EA021204B1 (ru) | 2015-04-30 |
| UY32169A (es) | 2010-04-30 |
| US20110195839A1 (en) | 2011-08-11 |
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