PROCESS FOR THE PREPARATION OF 1,4-DIHYDROPYRIDINES AND NOVEL 1,4-DIHYDROPYRIDINES USEFUL AS THERAPEUTIC AGENTS
The present invention provides a process for the preparation of 1,4-dihydropyridines of the formula (1), wherein R>1< IS H, NO>2<, CL, OAC, OH, R>2< IS H, NO>2<, CL, -O-CH>2<-O-, OMe, OAc, OEt, OH, R>3< IS H, NO>2<, CL, N(ME)>2<, -O- CH>2< -O-, O...
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Main Authors | , , , , |
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Format | Patent |
Language | English French |
Published |
04.12.2003
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Edition | 7 |
Subjects | |
Online Access | Get full text |
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Abstract | The present invention provides a process for the preparation of 1,4-dihydropyridines of the formula (1), wherein R>1< IS H, NO>2<, CL, OAC, OH, R>2< IS H, NO>2<, CL, -O-CH>2<-O-, OMe, OAc, OEt, OH, R>3< IS H, NO>2<, CL, N(ME)>2<, -O- CH>2< -O-, OME, OAC, OH, R>4< IS H, OME, OAC, OH, R>5< IS H, CL, I, AND R>6< AND R>7< are either methyl, ethyl or both by preparing a mixture of an aromatic aldehyde, alkyl acetoacetate and a source of ammonia, adsorbing the prepared mixture and adsorbent till adsorbent becomes free flowing, heating the material so obtained under microwave irradiation, cooling the reaction mixture and recovering the compound of formula (1). The present invention also relates to novel 1,4-dihydropyridines with cardiovascular activity.
L'invention concerne un procédé de préparation de 1,4-dihydropyridines de formule (1), dans laquelle : R1 représente H, NO2, Cl, OAc, OH ; R2 représente H, NO2, Cl, -O-CH2-O-, OMe, OAc, OEt, OH ; R3 représente H, NO2, Cl, N(Me)2, -O-CH2 -O-, OMe, OAc, OH ; R4 représente H, OMe, OAc, OH ; R5 représente H, Cl, l ; et R6 et R7 représentent méthyle, éthyle ou les deux. Ledit procédé consiste à préparer un mélange d'aldéhyde aromatique, d'acétoacétate d'alkyle et d'une source d'ammoniac ; à adsorber le mélange préparé sur l'adsorbant jusqu'à ce que ce dernier s'écoule facilement ; à chauffer le matériau ainsi obtenu par irradiation par micro-ondes ; à refroidir ledit mélange réactionnel et à récupérer le composé de formule (1). L'invention porte également sur des nouvelles 1,4-dihydropyridines agissant sur l'appareil cardiovasculaire. |
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AbstractList | The present invention provides a process for the preparation of 1,4-dihydropyridines of the formula (1), wherein R>1< IS H, NO>2<, CL, OAC, OH, R>2< IS H, NO>2<, CL, -O-CH>2<-O-, OMe, OAc, OEt, OH, R>3< IS H, NO>2<, CL, N(ME)>2<, -O- CH>2< -O-, OME, OAC, OH, R>4< IS H, OME, OAC, OH, R>5< IS H, CL, I, AND R>6< AND R>7< are either methyl, ethyl or both by preparing a mixture of an aromatic aldehyde, alkyl acetoacetate and a source of ammonia, adsorbing the prepared mixture and adsorbent till adsorbent becomes free flowing, heating the material so obtained under microwave irradiation, cooling the reaction mixture and recovering the compound of formula (1). The present invention also relates to novel 1,4-dihydropyridines with cardiovascular activity.
L'invention concerne un procédé de préparation de 1,4-dihydropyridines de formule (1), dans laquelle : R1 représente H, NO2, Cl, OAc, OH ; R2 représente H, NO2, Cl, -O-CH2-O-, OMe, OAc, OEt, OH ; R3 représente H, NO2, Cl, N(Me)2, -O-CH2 -O-, OMe, OAc, OH ; R4 représente H, OMe, OAc, OH ; R5 représente H, Cl, l ; et R6 et R7 représentent méthyle, éthyle ou les deux. Ledit procédé consiste à préparer un mélange d'aldéhyde aromatique, d'acétoacétate d'alkyle et d'une source d'ammoniac ; à adsorber le mélange préparé sur l'adsorbant jusqu'à ce que ce dernier s'écoule facilement ; à chauffer le matériau ainsi obtenu par irradiation par micro-ondes ; à refroidir ledit mélange réactionnel et à récupérer le composé de formule (1). L'invention porte également sur des nouvelles 1,4-dihydropyridines agissant sur l'appareil cardiovasculaire. |
Author | KHAJURIA, RAVI, KANT DHAR, KANAYA, LAL MAHENDROO, NEERAJ KAPOOR, VIJAY, KUMAR BEDI, KASTURI, LAL |
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DocumentTitleAlternate | PROCEDE DE PREPARATION DE 1,4-DIHYDROPYRIDINES ET NOUVELLES 1,4-DIHYDROPYRIDINES UTILES EN TANT QU'AGENTS THERAPEUTIQUES |
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Snippet | The present invention provides a process for the preparation of 1,4-dihydropyridines of the formula (1), wherein R>1< IS H, NO>2<, CL, OAC, OH, R>2< IS H,... |
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Title | PROCESS FOR THE PREPARATION OF 1,4-DIHYDROPYRIDINES AND NOVEL 1,4-DIHYDROPYRIDINES USEFUL AS THERAPEUTIC AGENTS |
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