AR030284A1 - Proceso para la sintesis de (2r, 2-alfa-r,3a) -2-[1-(3,5-bis(trifluorometil) fenil) etoxi]-3-(4-fluorofenil)-1,4-oxazina; dicho compuesto y sus formas polimorficas - Google Patents
Proceso para la sintesis de (2r, 2-alfa-r,3a) -2-[1-(3,5-bis(trifluorometil) fenil) etoxi]-3-(4-fluorofenil)-1,4-oxazina; dicho compuesto y sus formas polimorficasInfo
- Publication number
- AR030284A1 AR030284A1 ARP010102562A ARP010102562A AR030284A1 AR 030284 A1 AR030284 A1 AR 030284A1 AR P010102562 A ARP010102562 A AR P010102562A AR P010102562 A ARP010102562 A AR P010102562A AR 030284 A1 AR030284 A1 AR 030284A1
- Authority
- AR
- Argentina
- Prior art keywords
- compound
- oxazine
- bis
- phenyl
- synthesis
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 8
- 238000000034 method Methods 0.000 title abstract 3
- 230000015572 biosynthetic process Effects 0.000 title abstract 2
- 238000003786 synthesis reaction Methods 0.000 title abstract 2
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical class [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 title 1
- 239000002904 solvent Substances 0.000 abstract 2
- 238000005984 hydrogenation reaction Methods 0.000 abstract 1
- 230000000144 pharmacologic effect Effects 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
- 239000003890 substance P antagonist Substances 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
- C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
- C07D265/32—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings with oxygen atoms directly attached to ring carbon atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Abstract
Se refiere el compuesto (2R,2-alfa-R, 3a)-2-[1-(3,5-bis(trifluorometil)fenil]eloxi-3-(4-fluorofenil)-1,4-oxazina formas polimorficas de este compuesto y procesos para su preparacion. Este compuesto es util como intermediario en la síntesis de compuestos que poseen actividad farmacologica como antagonista del receptor de sustancia P. El proceso comprende poner en contacto un compuesto de la formula: (1) con un compuesto de la formula (2) en el cual Y se selecciona entre MgCI, MgBr, MgI y Li, en un primer solvente seguido por hidrogenacion, en un segundo solvente para dar el compuestos de la formula (3)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US21020300P | 2000-06-08 | 2000-06-08 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR030284A1 true AR030284A1 (es) | 2003-08-20 |
Family
ID=22781976
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP010102562A AR030284A1 (es) | 2000-06-08 | 2001-05-29 | Proceso para la sintesis de (2r, 2-alfa-r,3a) -2-[1-(3,5-bis(trifluorometil) fenil) etoxi]-3-(4-fluorofenil)-1,4-oxazina; dicho compuesto y sus formas polimorficas |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US6600040B2 (es) |
| EP (1) | EP1292584A1 (es) |
| JP (1) | JP2003535852A (es) |
| KR (1) | KR20030007887A (es) |
| CN (1) | CN1182125C (es) |
| AR (1) | AR030284A1 (es) |
| AU (1) | AU2001268170A1 (es) |
| BR (1) | BR0111472A (es) |
| CA (1) | CA2410404A1 (es) |
| CZ (1) | CZ20024013A3 (es) |
| EA (1) | EA004743B1 (es) |
| HR (1) | HRP20020973A2 (es) |
| HU (1) | HUP0400491A2 (es) |
| IL (1) | IL152793A0 (es) |
| MX (1) | MXPA02012101A (es) |
| NZ (1) | NZ523389A (es) |
| PL (1) | PL359137A1 (es) |
| SK (1) | SK17082002A3 (es) |
| WO (1) | WO2001094324A1 (es) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1292583A4 (en) * | 2000-06-08 | 2004-02-25 | Merck & Co Inc | METHOD FOR PRODUCING (2R, 2-ALPHA-R) -4-BENZYL-2- 1- (3,5-BIS (TRIFLUOROMETHYL) PHENYL) ETHOXY] -1,4-OXAZIN-3-ON |
| FR2876101B1 (fr) * | 2004-10-05 | 2007-03-02 | Sidem Pharma Sa Sa | Procede de preparation enantioselective de derives de sulfoxydes |
| WO2012146692A1 (en) | 2011-04-29 | 2012-11-01 | Sandoz Ag | Novel intermediates for the preparation of highly pure aprepitant or fosaprepitant |
| CN103012305B (zh) * | 2011-09-23 | 2016-08-17 | 江苏豪森药业集团有限公司 | 一种福沙匹坦中间体的制备方法 |
| CN103030668B (zh) * | 2011-10-09 | 2016-06-15 | 江苏豪森药业集团有限公司 | 一种制备福沙匹坦二甲葡胺的方法 |
| CZ304770B6 (cs) | 2012-03-13 | 2014-10-08 | Zentiva, K.S. | Způsob výroby 3-(((2R,3S)-2-((R)-1-(3,5-bis(trifluormethyl)fenyl)ethoxy)-3-(4-fluorfenyl)morfolino)methyl)-1H-1,2,4-triazol-5(4H)-onu (Aprepitantu) v polymorfní formě II |
| CN102675240B (zh) | 2012-04-13 | 2015-01-14 | 浙江海正药业股份有限公司 | 4-取代基-2-羟基吗啉-3-酮及其制备方法 |
| CN104327009B (zh) * | 2014-09-24 | 2016-07-20 | 山东省生物医药科学院 | 一种阿瑞匹坦关键中间体的精制方法 |
| CN104447607B (zh) * | 2014-12-12 | 2017-02-22 | 瑞阳制药有限公司 | 阿瑞匹坦中间体的制备方法 |
| CN104557760A (zh) * | 2015-01-28 | 2015-04-29 | 武汉励合生物医药科技有限公司 | 阿瑞吡坦中间体的制备方法 |
| CN106397349A (zh) * | 2016-08-31 | 2017-02-15 | 安徽省润生医药股份有限公司 | 一种阿瑞吡坦中间体及其制备方法 |
| CN109516964B (zh) * | 2017-09-19 | 2022-05-31 | 鲁南制药集团股份有限公司 | 一种阿瑞匹坦中间体的制备方法 |
| CN109694360A (zh) * | 2018-12-28 | 2019-04-30 | 凯瑞斯德生化(苏州)有限公司 | 一种阿瑞匹坦中间体的制备方法 |
| CN110746371B (zh) * | 2019-11-20 | 2022-07-15 | 山东鲁抗医药股份有限公司 | 制备阿瑞匹坦的中间体及其制备方法与应用 |
| CN114235340B (zh) * | 2020-06-09 | 2023-11-10 | 重庆交通大学 | 河道泡漩结构跟踪方法及通航预警方法 |
| CN111829749B (zh) * | 2020-07-27 | 2024-11-08 | 中国空气动力研究与发展中心高速空气动力研究所 | 一种用于风洞超声速流校大行程单点移测装置及布线方法 |
| CN113582982B (zh) * | 2021-06-15 | 2023-06-16 | 山东罗欣药业集团股份有限公司 | 一种nk1受体拮抗剂的制备方法 |
| CN120027863B (zh) * | 2025-04-22 | 2025-07-15 | 四川交通职业技术学院 | 一种高速公路施工桥隧安全监测装置 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5719147A (en) * | 1992-06-29 | 1998-02-17 | Merck & Co., Inc. | Morpholine and thiomorpholine tachykinin receptor antagonists |
| IL111960A (en) * | 1993-12-17 | 1999-12-22 | Merck & Co Inc | Morpholines and thiomorpholines their preparation and pharmaceutical compositions containing them |
| CN1067683C (zh) | 1993-12-29 | 2001-06-27 | 默克·夏普-道姆公司 | 取代的吗啉衍生物及其作为治疗剂的用途 |
| ZA985765B (en) | 1997-07-02 | 1999-08-04 | Merck & Co Inc | Polymorphic form of a tachykinin receptor antagonist. |
| GB9813025D0 (en) | 1998-06-16 | 1998-08-12 | Merck Sharp & Dohme | Chemical synthesis |
| JP2002524556A (ja) * | 1998-09-11 | 2002-08-06 | メルク エンド カムパニー インコーポレーテッド | Ｎ−ベンジル−３−（４−フルオロフェニル）−１，４−オキサジン−２−オンの合成方法 |
| AU1230000A (en) * | 1998-10-30 | 2000-05-22 | Merck & Co., Inc. | Linear process for the preparation of a morpholine compound |
| AU1233000A (en) | 1998-10-30 | 2000-05-22 | Merck & Co., Inc. | Process for the preparation of 2-(r)-(1- (r)-(3,5-bis (trifluoromethyl) phenyl)ethoxy) -4-((5-dimethylaminomethyl) -1,2,3-triazol -4-yl)methyl) -3-(s)-(4- fluorophenyl) morpholine |
| AU764492B2 (en) * | 1998-12-29 | 2003-08-21 | Pharmacia & Upjohn Company | Method for the preparation of aryl ethers |
-
2001
- 2001-05-29 AR ARP010102562A patent/AR030284A1/es not_active Application Discontinuation
- 2001-06-04 HU HU0400491A patent/HUP0400491A2/hu unknown
- 2001-06-04 BR BR0111472-7A patent/BR0111472A/pt not_active IP Right Cessation
- 2001-06-04 CN CNB018108962A patent/CN1182125C/zh not_active Expired - Fee Related
- 2001-06-04 WO PCT/US2001/018042 patent/WO2001094324A1/en not_active Ceased
- 2001-06-04 AU AU2001268170A patent/AU2001268170A1/en not_active Abandoned
- 2001-06-04 PL PL01359137A patent/PL359137A1/xx unknown
- 2001-06-04 CZ CZ20024013A patent/CZ20024013A3/cs unknown
- 2001-06-04 SK SK1708-2002A patent/SK17082002A3/sk not_active Application Discontinuation
- 2001-06-04 HR HR20020973A patent/HRP20020973A2/xx not_active Application Discontinuation
- 2001-06-04 KR KR1020027016609A patent/KR20030007887A/ko not_active Withdrawn
- 2001-06-04 MX MXPA02012101A patent/MXPA02012101A/es unknown
- 2001-06-04 JP JP2002501874A patent/JP2003535852A/ja not_active Withdrawn
- 2001-06-04 IL IL15279301A patent/IL152793A0/xx unknown
- 2001-06-04 CA CA002410404A patent/CA2410404A1/en not_active Abandoned
- 2001-06-04 NZ NZ523389A patent/NZ523389A/en unknown
- 2001-06-04 EA EA200300002A patent/EA004743B1/ru not_active IP Right Cessation
- 2001-06-04 EP EP01946075A patent/EP1292584A1/en not_active Withdrawn
- 2001-06-08 US US09/878,042 patent/US6600040B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| MXPA02012101A (es) | 2003-04-25 |
| US6600040B2 (en) | 2003-07-29 |
| SK17082002A3 (sk) | 2003-04-01 |
| NZ523389A (en) | 2004-08-27 |
| AU2001268170A1 (en) | 2001-12-17 |
| EP1292584A1 (en) | 2003-03-19 |
| HRP20020973A2 (en) | 2005-02-28 |
| HUP0400491A2 (hu) | 2004-06-28 |
| EA004743B1 (ru) | 2004-08-26 |
| IL152793A0 (en) | 2003-06-24 |
| CN1182125C (zh) | 2004-12-29 |
| BR0111472A (pt) | 2004-01-06 |
| PL359137A1 (en) | 2004-08-23 |
| CA2410404A1 (en) | 2001-12-13 |
| JP2003535852A (ja) | 2003-12-02 |
| CN1436178A (zh) | 2003-08-13 |
| EA200300002A1 (ru) | 2003-04-24 |
| US20020052494A1 (en) | 2002-05-02 |
| CZ20024013A3 (cs) | 2003-03-12 |
| KR20030007887A (ko) | 2003-01-23 |
| WO2001094324A1 (en) | 2001-12-13 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |