ES481038A1 - Un procedimiento para la preparacion de 2,4-diamino-5-bencil-pirimidinas - Google Patents
Un procedimiento para la preparacion de 2,4-diamino-5-bencil-pirimidinasInfo
- Publication number
- ES481038A1 ES481038A1 ES481038A ES481038A ES481038A1 ES 481038 A1 ES481038 A1 ES 481038A1 ES 481038 A ES481038 A ES 481038A ES 481038 A ES481038 A ES 481038A ES 481038 A1 ES481038 A1 ES 481038A1
- Authority
- ES
- Spain
- Prior art keywords
- so2r
- alkyllithium
- alkylthio
- alkoxy
- hydrogen
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/32—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07D207/325—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
- C07D207/327—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
- C07C323/22—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and doubly-bound oxygen atoms bound to the same carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C329/00—Thiocarbonic acids; Halides, esters or anhydrides thereof
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C333/00—Derivatives of thiocarbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
- C07C333/02—Monothiocarbamic acids; Derivatives thereof
- C07C333/08—Monothiocarbamic acids; Derivatives thereof having nitrogen atoms of thiocarbamic groups bound to carbon atoms of six-membered aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
- C07D239/49—Two nitrogen atoms with an aralkyl radical, or substituted aralkyl radical, attached in position 5, e.g. trimethoprim
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D295/145—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Macromolecular Compounds Obtained By Forming Nitrogen-Containing Linkages In General (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Un procedimiento para la preparación de 2,4- diamino-5-bencil-pirimidina, de la fórmula general **(Fórmula-01)** en la que R1 representa hidrógeno o alquilo de C1-6'' R2 representa hidrógeno, R3 representa mercapto, alquilitio de C1-6'' carboxi-alquilitio de C1-6'', alcoxilo de C1-6- alquilitio de C1-6'' dimetilcabamoiltio, -S(O)R'' o -SO2R'' y R4 representa alquilitio de C1-6'' -S(O)R'' o - SO2R''; o bien R1 representa hidrógeno, R2 y R4 representa alquilitio de C1-6'' -S(O)R'' o - SO2R'' y R3 representa alcoxilo de C1-6'', mercapto, alquilitio de C1-6'' carboxi-alquilitio de C1-6, dimetilcarbamoiltio, -S(O)R'', - SO2R'' o -NR"R"''; o bien R1 representa hidrógeno, R2 representa alcoxilo de C1-6'' R3 representa mercapto, alquilitio de C1-6'' carboxi-alquilitio de C1-6'' alcoxilo de C1- 6''alquilitio de C1-6'' dimetilcarbamoiltio, -S(o)R'' o -SO2R'' y R4 representa alquilitio de C1-6'' -S(o)R'' o - SO2R''; o bien R1 representa hidrógeno, R2 representa halógeno, R3 representa alquilitio de C1-6'' -S(O)R'' o - SO2R'' y R4 representa alquilitio de C1-6'' -S(O)R'' o - SO2R''; o bien R1 representa hidrógeno, R2 representa halógeno o alcoxilo de C1-6'' R3 representa mercapto, alquilitio de C1-6'' carboxi-alquilitio de C1-6'' carboalcoxi-alquilitio de C1-6'' ciano-alquilitio de C1-6'' alcoxilo de C1- 6-alquilitio de C1-6'' alcoxilo de C1-6'' alquilitio de C1-6'' dimetilcarbamoiltio, -S(O)R'' o - SO2R'' y R4 significa halógeno o alcoxilo de C1-6; R'' representa alquilo de C1-6 y R" y R"'' representan, independientemente uno de otro, hidrógeno o alquilo de C1-6'' o bien, juntos, alquileno de C2-6 (eventualmente con 1 a 3 enlaces dobles), y sus sales compatibles fisiológicamente, caracterizado porque se elimina reductivamente el sustituyente X en un compuesto de la fórmula **(Fórmula-02)** en donde X significa halógeno R1, R2, R3, y R4 tienen el significado antes indicado, y si se desea, se convierte el compuesto obtenido en una sal fisiológicamente compatible.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| LU78487 | 1977-11-10 | ||
| CH977678 | 1978-09-19 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES481038A1 true ES481038A1 (es) | 1980-04-01 |
Family
ID=25705315
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES474921A Expired ES474921A1 (es) | 1977-11-10 | 1978-11-08 | Un procedimiento para la preparacion de 2,4-diamino-5-bencil-pirimidinas |
| ES481038A Expired ES481038A1 (es) | 1977-11-10 | 1979-05-16 | Un procedimiento para la preparacion de 2,4-diamino-5-bencil-pirimidinas |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES474921A Expired ES474921A1 (es) | 1977-11-10 | 1978-11-08 | Un procedimiento para la preparacion de 2,4-diamino-5-bencil-pirimidinas |
Country Status (22)
| Country | Link |
|---|---|
| EP (3) | EP0032395B1 (es) |
| JP (1) | JPS5476586A (es) |
| AR (2) | AR228423A1 (es) |
| AT (1) | AT359070B (es) |
| AU (1) | AU527943B2 (es) |
| BR (1) | BR7807425A (es) |
| CA (1) | CA1108611A (es) |
| DE (1) | DE2847825A1 (es) |
| DK (1) | DK144418C (es) |
| ES (2) | ES474921A1 (es) |
| FI (1) | FI783368A7 (es) |
| FR (4) | FR2422647A1 (es) |
| GB (3) | GB2086882B (es) |
| GR (1) | GR71725B (es) |
| IL (1) | IL55869A (es) |
| IT (1) | IT1100210B (es) |
| MC (1) | MC1222A1 (es) |
| NL (1) | NL7811170A (es) |
| NO (1) | NO783775L (es) |
| PH (1) | PH15918A (es) |
| PT (1) | PT68773A (es) |
| SE (1) | SE7811593L (es) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IT1138146B (it) * | 1981-08-11 | 1986-09-17 | Proter Spa | Processo per la produzione della 2,4-diammino-(3,5-dimetossi-4-metos sietossi-benzil)-pirimidina |
| JPS5888368A (ja) * | 1981-11-09 | 1983-05-26 | ザ・ウエルカム・フアウンデ−シヨン・リミテツド | ベンジルピリミジン誘導体の製造法 |
| DE3304202A1 (de) * | 1983-02-08 | 1984-08-09 | Bayer Ag, 5090 Leverkusen | Verfahren zur herstellung von aromatischen aldehyden |
| DE3603577A1 (de) * | 1986-02-06 | 1987-08-13 | Joachim K Prof Dr Seydel | Neue substituierte 2,4-diamino-5-benzylpyrimidine, deren herstellung und deren verwendung als arzneimittel mit antibakterieller wirksamkeit |
| JPH07509215A (ja) * | 1990-11-14 | 1995-10-12 | カイロン コーポレイション | ジヒドロ葉酸還元酵素の特異的阻害およびそのための化合物 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE2165362A1 (de) * | 1970-12-29 | 1972-07-27 | Nisshin Flour Milling Co. Ltd., Tokio | .-Verfahren zur Herstellung von Pyrimidinderivaten |
| NL7200058A (es) * | 1971-01-21 | 1972-07-25 | ||
| IL38276A (en) * | 1971-12-01 | 1976-09-30 | Plantex Ltd | Process for the preparation of 2,4-diamino-5-substituted benzylpyrimidines |
| BE798724A (fr) * | 1973-04-26 | 1973-08-16 | En Abrege Socechim Soc Et Chim | Nouveaux composes chimiques |
| DK136470B (da) * | 1973-11-08 | 1977-10-17 | Hoffmann La Roche | Analogifremgangsmåde til fremstilling af 2,4-diamino-5-benzylpyrimidinderivater eller salte deraf. |
| CH605828A5 (es) * | 1974-12-24 | 1978-10-13 | Hoffmann La Roche | |
| DE2635765C3 (de) * | 1976-08-09 | 1979-02-08 | Ludwig Heumann & Co Gmbh, 8500 Nuernberg | Verfahren zur Herstellung von 2,4-EMamino-5-(3',4'r5'-trimethoxybenzyl)-pyrimidin |
-
1978
- 1978-04-08 GR GR57610A patent/GR71725B/el unknown
- 1978-11-03 IL IL55869A patent/IL55869A/xx unknown
- 1978-11-03 DE DE19782847825 patent/DE2847825A1/de not_active Withdrawn
- 1978-11-03 EP EP81100161A patent/EP0032395B1/de not_active Expired
- 1978-11-03 EP EP81100160A patent/EP0035624B1/de not_active Expired
- 1978-11-03 EP EP78101300A patent/EP0003212B1/de not_active Expired
- 1978-11-03 AU AU41323/78A patent/AU527943B2/en not_active Expired
- 1978-11-06 FI FI783368A patent/FI783368A7/fi unknown
- 1978-11-06 CA CA315,867A patent/CA1108611A/en not_active Expired
- 1978-11-07 MC MC781339A patent/MC1222A1/fr unknown
- 1978-11-08 FR FR7831549A patent/FR2422647A1/fr active Granted
- 1978-11-08 ES ES474921A patent/ES474921A1/es not_active Expired
- 1978-11-09 IT IT29638/78A patent/IT1100210B/it active
- 1978-11-09 GB GB8114950A patent/GB2086882B/en not_active Expired
- 1978-11-09 PT PT68773A patent/PT68773A/pt unknown
- 1978-11-09 GB GB7843861A patent/GB2007669B/en not_active Expired
- 1978-11-09 SE SE7811593A patent/SE7811593L/xx unknown
- 1978-11-09 AT AT803378A patent/AT359070B/de not_active IP Right Cessation
- 1978-11-09 NO NO783775A patent/NO783775L/no unknown
- 1978-11-09 GB GB8114951A patent/GB2087378B/en not_active Expired
- 1978-11-09 JP JP13740378A patent/JPS5476586A/ja active Pending
- 1978-11-09 DK DK500178A patent/DK144418C/da not_active IP Right Cessation
- 1978-11-10 AR AR274416A patent/AR228423A1/es active
- 1978-11-10 NL NL7811170A patent/NL7811170A/xx not_active Application Discontinuation
- 1978-11-10 PH PH21791A patent/PH15918A/en unknown
- 1978-11-10 BR BR7807425A patent/BR7807425A/pt unknown
-
1979
- 1979-05-16 ES ES481038A patent/ES481038A1/es not_active Expired
- 1979-06-22 FR FR7916099A patent/FR2422404A1/fr active Granted
- 1979-06-22 FR FR7916101A patent/FR2422648A1/fr active Granted
- 1979-06-22 FR FR7916100A patent/FR2422632A1/fr active Granted
- 1979-08-09 AR AR277656A patent/AR222831A1/es active
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