CU21022L - New benzylpyrymidins - Google Patents
New benzylpyrymidinsInfo
- Publication number
- CU21022L CU21022L CU7434115A CU34115A CU21022L CU 21022 L CU21022 L CU 21022L CU 7434115 A CU7434115 A CU 7434115A CU 34115 A CU34115 A CU 34115A CU 21022 L CU21022 L CU 21022L
- Authority
- CU
- Cuba
- Prior art keywords
- group
- compound
- formula
- amino
- meaning
- Prior art date
Links
Classifications
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- 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
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- 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
- C07C255/00—Carboxylic acid nitriles
-
- 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
-
- 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
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- 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
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- 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
- C07D295/155—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 separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Oncology (AREA)
- Pharmacology & Pharmacy (AREA)
- Communicable Diseases (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyrrole Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
nta un grupo -N(NO)R4, con Zn/CH3COOH, o bien i) someter un compuesto de la fórmula I, en donde n sigUn procedimiento para la preparación de derivados de bencil-pirimidina de la fórmula general (I) en la que R1 y R2 representan cada uno, independientemente un grupo de alquilo C1-3´ alcoxilo de C1-3´ alquenilo de C2-3 o alqueniloxilo de C2-3´ Z representa un grupo nitro, amino, pirrolo, pirrolidino, piperidino, -NHR , -NHR5, -N(R4) (R5), -NH4COOR4, -NHCOOR4 , -NHCONHR3 , -NHCSNHR5, -N=N-N8R4)2, -N8NO)4 o -NR·-NH2, R4 representa un grupo de alquilo de C1-3 o alquenilo de C2-3´ R5 representa un grupo de acilo, R3 representa un átomo de hidrógeno o un grupo de alquilo de C1-3 o alquenilo de C2-3´ A representa un átomo de oxígeno enlazado a uno de los átomos de nitrógeno cíclicos y n significa cero o 1, y sus sales, cuyo procedimiento comprende a) hacer reaccionar un compuesto de la fórmula general (IIa) o bién (fórmula IIb) en donde Z representa un grupo nitro, amino, pirrolo, pirrolidino, piperidino, -NHR4, -N(R4)2´ -NHR5, -N(R4) (R5), -NR4COOR4, _NHCOOR4, -NHCONHR3, -NHCSNHR3 o -NR3NH2, el símbolo R6 representa un grupo de alquilo inferior o los dos símbolos R6 juntos representan un grupo de alquileno inferior, y representa un grupo partiente y R1, R2, R3, R4 y R5 tienen el significado indicado en esta reinvidicación 1, con guanidina, o b) hacer reaccionar un compuesto de la fórmula general (III) en la que X representa un átomo de cloro o de bromo o un grupo alquilmercapto, alquilsulfonilo o amino, con la salvedad de que uno de los símbolos X, por lo menos, tenga un significado distinto a un grupo amino, R1 y R2 tienen el significado expuesto en esta reivindicación 1, y Z tiene el significado antes expuesto en esta reivindicación, con amoníaco, o bien c) eliminar reductivamente el substitúyete designado con X1 en un compuesto de la fórmula general (IV) en la que X1 representa un átomo de cloro o de bromo o un grupo hidroxílico, R1, R2 tienen el significado expuesto en esta reivindicación 1 y Z1 tiene el significado antes expuesto en esta reivindicación, o bien d) diazoar un compuesto de la fórmula I, en donde Z representa un grupo amino, y haciendo reaccionar a continuación el producto con azida sódica, con una amina de la fórmula NH(R4)2 o con un sulfito alcalino, o bien e) tratar un compuesto de la fórmula I, en donde Z representa un grupo NHR4, con ácido nítrico, o bien f) convertir el grupo Z2 en un compuesto de la fórmula general (Va) (Vb) 0 bien (Vc) en donde R1 y R2 tienen el significado indicado en esta reivindicación 1, y Z2, que puede ser igual o diferente en las fórmulas Vb y Vc, representa un grupo convertible por reducción o hidrólisis en un grupo amino o un grupo -NHR4, en un grupo amino o un grupo -NHR4, o bien g) alquilar o alquenilar el grupo designado con Z3 en un compuesto de la fórmula general (Ia) en la que Z3 representa un grupo -NHR5 o -NHCOOR4 y R1, R2, R4 y R5 tienen el significado indicado en esta reivindicación 1, o bien h) reducir un compuesto de la fórmula I, en donde Z represenifica cero, a N-oxidación y, si se desea, convertir un compuesto de la fórmula I obtenido en una sal
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CH1305773A CH591456A5 (es) | 1973-09-12 | 1973-09-12 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CU21022L true CU21022L (en) | 1981-09-09 |
| CU34115A CU34115A (es) | 1983-10-04 |
Family
ID=4388903
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CU34115A CU34115A (es) | 1973-09-12 | 1974-09-11 | Nuevas bencilpirimidinas |
Country Status (28)
| Country | Link |
|---|---|
| JP (1) | JPS6042238B2 (es) |
| AR (2) | AR207764A1 (es) |
| AT (1) | AT338797B (es) |
| BE (1) | BE819773A (es) |
| BR (1) | BR7407614D0 (es) |
| CA (1) | CA1037476A (es) |
| CH (1) | CH591456A5 (es) |
| CU (1) | CU34115A (es) |
| DD (2) | DD116824A5 (es) |
| DE (1) | DE2443682C2 (es) |
| DK (1) | DK135683B (es) |
| ES (7) | ES429949A1 (es) |
| FI (1) | FI58638C (es) |
| FR (1) | FR2242984B1 (es) |
| GB (3) | GB1484483A (es) |
| HK (1) | HK181A (es) |
| HU (1) | HU170427B (es) |
| IE (1) | IE40523B1 (es) |
| IL (1) | IL45510A (es) |
| LU (1) | LU70878A1 (es) |
| NL (1) | NL155827B (es) |
| NO (1) | NO140858C (es) |
| PH (1) | PH10643A (es) |
| PL (2) | PL99159B1 (es) |
| SE (1) | SE419443B (es) |
| SU (3) | SU577987A3 (es) |
| YU (3) | YU217874A (es) |
| ZA (1) | ZA745317B (es) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4515948A (en) * | 1973-09-12 | 1985-05-07 | Hoffmann-La Roche Inc. | 2,4-Diamino-5-(4-amino and 4-dimethylamino-3,5-dimethoxy benzyl)pyrimidines |
| EP0001633A1 (en) * | 1977-10-18 | 1979-05-02 | The Wellcome Foundation Limited | Processes for preparing tri-heterocyclic substituted methanes and their conversion into further intermediates useful in the preparation of pharmacologically active compounds |
| CH639273A5 (de) * | 1978-09-12 | 1983-11-15 | Hoffmann La Roche | Diuretische mittel. |
| 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 |
| DE3250132C2 (de) * | 1981-11-09 | 1997-01-16 | Mallinckrodt Veterinary Inc | Verfahren zur Herstellung von 2,4-Diamino-5-benzyl-pyrimidinen und neue Zwischenprodukte des Verfahrens |
| GB2180836A (en) * | 1985-09-27 | 1987-04-08 | William James Stephen Barker | Sunscreen |
| CA1300166C (en) * | 1987-12-03 | 1992-05-05 | Alfredo Guerrato | Process for the preparation of a benzoic acid ester |
| US4900859A (en) * | 1987-12-03 | 1990-02-13 | Hoffman-La Roche Inc. | Process for 4-dimethylamino-3,5-dimethoxybenzaldehyde |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE1103931B (de) * | 1957-02-21 | 1961-04-06 | Wellcome Found | Verfahren zur Herstellung von 2, 4-Diamino-5-benzylpyrimidinderivaten |
| US3485840A (en) * | 1964-11-12 | 1969-12-23 | Hoffmann La Roche | 2,4-diamino - 5 - (2',4',5'-substituted benzyl) pyrimidines,intermediates and processes |
-
1973
- 1973-09-12 CH CH1305773A patent/CH591456A5/xx not_active IP Right Cessation
-
1974
- 1974-01-01 AR AR255569A patent/AR207764A1/es active
- 1974-08-06 YU YU02178/74A patent/YU217874A/xx unknown
- 1974-08-19 ZA ZA00745317A patent/ZA745317B/xx unknown
- 1974-08-21 IL IL45510A patent/IL45510A/xx unknown
- 1974-08-21 CA CA207,509A patent/CA1037476A/en not_active Expired
- 1974-09-02 FI FI2561/74A patent/FI58638C/fi active
- 1974-09-03 NL NL7411685.A patent/NL155827B/xx not_active IP Right Cessation
- 1974-09-04 DK DK468374AA patent/DK135683B/da unknown
- 1974-09-06 PL PL1974195308A patent/PL99159B1/pl unknown
- 1974-09-06 PL PL1974173909A patent/PL97757B1/pl unknown
- 1974-09-09 PH PH16253A patent/PH10643A/en unknown
- 1974-09-09 SE SE7411382A patent/SE419443B/xx unknown
- 1974-09-09 IE IE1870/74A patent/IE40523B1/xx unknown
- 1974-09-10 DD DD181015A patent/DD116824A5/xx unknown
- 1974-09-10 LU LU70878A patent/LU70878A1/xx unknown
- 1974-09-10 JP JP49103536A patent/JPS6042238B2/ja not_active Expired
- 1974-09-10 FR FR7430568A patent/FR2242984B1/fr not_active Expired
- 1974-09-10 DD DD190238A patent/DD122785A5/xx unknown
- 1974-09-11 ES ES429949A patent/ES429949A1/es not_active Expired
- 1974-09-11 GB GB47894/76A patent/GB1484483A/en not_active Expired
- 1974-09-11 GB GB39617/74A patent/GB1484481A/en not_active Expired
- 1974-09-11 SU SU7402058406A patent/SU577987A3/ru active
- 1974-09-11 GB GB47893/76A patent/GB1484482A/en not_active Expired
- 1974-09-11 NO NO743271A patent/NO140858C/no unknown
- 1974-09-11 BE BE148396A patent/BE819773A/xx not_active IP Right Cessation
- 1974-09-11 HU HUHO1718A patent/HU170427B/hu not_active IP Right Cessation
- 1974-09-11 AT AT735174A patent/AT338797B/de not_active IP Right Cessation
- 1974-09-11 CU CU34115A patent/CU34115A/es unknown
- 1974-09-12 DE DE2443682A patent/DE2443682C2/de not_active Expired
- 1974-09-12 BR BR7614/74A patent/BR7407614D0/pt unknown
-
1975
- 1975-04-25 ES ES437011A patent/ES437011A1/es not_active Expired
- 1975-04-25 ES ES437009A patent/ES437009A1/es not_active Expired
- 1975-04-25 ES ES437007A patent/ES437007A1/es not_active Expired
- 1975-04-25 ES ES437012A patent/ES437012A1/es not_active Expired
- 1975-04-25 ES ES437008A patent/ES437008A1/es not_active Expired
- 1975-04-25 ES ES437013A patent/ES437013A1/es not_active Expired
- 1975-06-20 SU SU752145937A patent/SU609465A3/ru active
- 1975-06-20 SU SU7502145932A patent/SU571189A3/ru active
- 1975-06-30 AR AR259408A patent/AR211387Q/es unknown
-
1980
- 1980-11-27 YU YU3015/80A patent/YU37153B/xx unknown
- 1980-11-27 YU YU3016/80A patent/YU37154B/xx unknown
-
1981
- 1981-01-08 HK HK1/81A patent/HK181A/xx unknown
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