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Papers by Jean-Pierre Geerts
Tetrahedron Letters, 1974
Ketenes bearing a-carbanion-stabilizing substituents are useful synthetic intermediates 192 offer... more Ketenes bearing a-carbanion-stabilizing substituents are useful synthetic intermediates 192 offering the interesting possibility of effecting the position-and stereospecific addition of two carbon-chains to an olefinic substrate (scheme 1).
NEW MATERIAL: Compd. of formula I (wherein R 1 and R 2 are each H, an alkyl; R 3 is H, an alkyl, ... more NEW MATERIAL: Compd. of formula I (wherein R 1 and R 2 are each H, an alkyl; R 3 is H, an alkyl, a hydroxyalkyl, NH 2 , OH; R 4 is H, an alkyl or R 3 and R 4 are each pyrrolidino, piperidino and morphorino together with bound N; R 5 and R 6 are each H, OH, an alkyl, an alkoxy and at least one is a group except H) and their optical isomers and racemic mixtures or acid additive salts thereof. EXAMPLE: 2-Hydroxy-3[(1H-imidazol-4-yl)methyl]-benzamide. USE: The compd. antiishemia to heart, cereb and tissue and properties of α 2 - adrenergic receptor agonist and are useful for remedy for angina pectoris, myocardial infarction and psychiatric disorder. PROCESS: E.g. alkyl 1(1H-imidazol-4-yl) alkyl-benzoate of formula II is reacted with a compd. of formula III to obtain a compd. of formula I. COPYRIGHT: (C)1989,JPO
Nouveaux 1-(1H-imidazol-4-yl)alkyl-benzamides substitues et leurs sels, leurs procedes de prepara... more Nouveaux 1-(1H-imidazol-4-yl)alkyl-benzamides substitues et leurs sels, leurs procedes de preparation et compositions therapeutiques. Ces composes repondant a la formule dans laquelle R₁, R₂ = hydrogene ou alkyle en C₁-C₄, R₃ = hydrogene, amino, hydroxyle, alkyle en C₁-C₄ ou hydroxyalkyle en C₁-C₄, R₄ = hydrogene ou alkyle en C₁-C₄, ou R₃R₄N = pyrrolidino, piperidino ou morpholino, R₅ et R₆ = hydrogene, hydroxyle, alkyle en C₁-C₄ ou alkoxy en C₁-C₄; au moins un des R₅ et R₆ ≠ hydrogene. Ces composes sont prepares soit par reaction d'un compose azote sur un 1-(1H-imidazol-4-yl)alkyl-benzoate d'alkyle ou sur un acide 1-(1H-imidazol-4-yl)alkyl-benzoique, soit par hydrolyse en milieu acide d'un 2-hydroxy-3-[1-(1H-imidazol-4-yl)alkyl]-benzonitrile. Ces composes possedent des activites anti-ischemiques et agoniste des recepteurs α₂-adrenergiques.
4-(1,2,3,4-tetrahydro-1-naphtalenyl)-1H-imidazoles et 4-(2,3-dihydro-1H-inden-1-yl)-1H-imidazoles... more 4-(1,2,3,4-tetrahydro-1-naphtalenyl)-1H-imidazoles et 4-(2,3-dihydro-1H-inden-1-yl)-1H-imidazoles substitues, leurs isomeres optiques et leurs melanges racemiques, leurs sels, leurs procedes de preparation et compositions therapeutiques les contenant. Ces composes repondent a la formule generale dans laquelle n = 1 ou 2, R 1 , R 2 , R 3 et R 4 , qui peuvent etre identiques ou differents, representent chacun un atome d'hydrogene ou d'halogene, un groupe hydroxyle, un radical alkyle ou alkoxy, et R 5 represente un atome d'hydrogene ou un radical alkyle, avec la restriction que R 1 , R 2 , R 3 , R 4 et R 5 ne peuvent etre simultanement de l'hydrogene lorsque n est egal a 2, les radicaux alkyle et alkoxy ayant de 1 a 4 atomes de carbone. Ce sont des composes nouveaux qui presentent des activites anti-ischemique et anti-hypertensive.
Tetrahedron Letters, 1974
Ketenes bearing a-carbanion-stabilizing substituents are useful synthetic intermediates 192 offer... more Ketenes bearing a-carbanion-stabilizing substituents are useful synthetic intermediates 192 offering the interesting possibility of effecting the position-and stereospecific addition of two carbon-chains to an olefinic substrate (scheme 1).
NEW MATERIAL: Compd. of formula I (wherein R 1 and R 2 are each H, an alkyl; R 3 is H, an alkyl, ... more NEW MATERIAL: Compd. of formula I (wherein R 1 and R 2 are each H, an alkyl; R 3 is H, an alkyl, a hydroxyalkyl, NH 2 , OH; R 4 is H, an alkyl or R 3 and R 4 are each pyrrolidino, piperidino and morphorino together with bound N; R 5 and R 6 are each H, OH, an alkyl, an alkoxy and at least one is a group except H) and their optical isomers and racemic mixtures or acid additive salts thereof. EXAMPLE: 2-Hydroxy-3[(1H-imidazol-4-yl)methyl]-benzamide. USE: The compd. antiishemia to heart, cereb and tissue and properties of α 2 - adrenergic receptor agonist and are useful for remedy for angina pectoris, myocardial infarction and psychiatric disorder. PROCESS: E.g. alkyl 1(1H-imidazol-4-yl) alkyl-benzoate of formula II is reacted with a compd. of formula III to obtain a compd. of formula I. COPYRIGHT: (C)1989,JPO
Nouveaux 1-(1H-imidazol-4-yl)alkyl-benzamides substitues et leurs sels, leurs procedes de prepara... more Nouveaux 1-(1H-imidazol-4-yl)alkyl-benzamides substitues et leurs sels, leurs procedes de preparation et compositions therapeutiques. Ces composes repondant a la formule dans laquelle R₁, R₂ = hydrogene ou alkyle en C₁-C₄, R₃ = hydrogene, amino, hydroxyle, alkyle en C₁-C₄ ou hydroxyalkyle en C₁-C₄, R₄ = hydrogene ou alkyle en C₁-C₄, ou R₃R₄N = pyrrolidino, piperidino ou morpholino, R₅ et R₆ = hydrogene, hydroxyle, alkyle en C₁-C₄ ou alkoxy en C₁-C₄; au moins un des R₅ et R₆ ≠ hydrogene. Ces composes sont prepares soit par reaction d'un compose azote sur un 1-(1H-imidazol-4-yl)alkyl-benzoate d'alkyle ou sur un acide 1-(1H-imidazol-4-yl)alkyl-benzoique, soit par hydrolyse en milieu acide d'un 2-hydroxy-3-[1-(1H-imidazol-4-yl)alkyl]-benzonitrile. Ces composes possedent des activites anti-ischemiques et agoniste des recepteurs α₂-adrenergiques.
4-(1,2,3,4-tetrahydro-1-naphtalenyl)-1H-imidazoles et 4-(2,3-dihydro-1H-inden-1-yl)-1H-imidazoles... more 4-(1,2,3,4-tetrahydro-1-naphtalenyl)-1H-imidazoles et 4-(2,3-dihydro-1H-inden-1-yl)-1H-imidazoles substitues, leurs isomeres optiques et leurs melanges racemiques, leurs sels, leurs procedes de preparation et compositions therapeutiques les contenant. Ces composes repondent a la formule generale dans laquelle n = 1 ou 2, R 1 , R 2 , R 3 et R 4 , qui peuvent etre identiques ou differents, representent chacun un atome d'hydrogene ou d'halogene, un groupe hydroxyle, un radical alkyle ou alkoxy, et R 5 represente un atome d'hydrogene ou un radical alkyle, avec la restriction que R 1 , R 2 , R 3 , R 4 et R 5 ne peuvent etre simultanement de l'hydrogene lorsque n est egal a 2, les radicaux alkyle et alkoxy ayant de 1 a 4 atomes de carbone. Ce sont des composes nouveaux qui presentent des activites anti-ischemique et anti-hypertensive.