Process for preparing 1,5-benzothiazepine derivative

Details Process for preparing 1,5-benzothiazepine derivative Process for preparing 1,5-benzothiazepine derivative

C - Chemistry, Metallurgy

07

D

C07D 281/02 (2006.01) C07C 323/36 (2006.01) C07C 323/60 (2006.01) C07D 207/27 (2006.01) C07D 211/76 (2006.01) C07D 231/12 (2006.01) C07D 233/61 (2006.01) C07D 249/08 (2006.01) C07D 265/22 (2006.01) C07D 281/10 (2006.01) C07D 295/155 (2006.01) C07D 303/48 (2006.01) C07D 405/06 (2006.01)

Patent

CA 2197816

A novel process for preparing 1,5-benzothiazepine derivative [II]: (see fig. II) wherein Ring A and Ring B are substituted or unsubstituted benzene ring, and R3 is H, (di-lower alkylamino)-lower alkyl or substituted or unsubstituted piperazinyl-lower alkyl, or a salt thereof, in high yield and in a single step from a novel 3-(2-amino-substituted or unsubstituted phenylthio)-2-hydroxy-3- substituted or unsubstituted phenylpropionamide compound. Said 1,5-benzothiazepine derivative [II] is useful as an intermediate for preparing medicaments such as diltiazem hydrochloride.

ouveau procédé pour préparer un dérivé de la 1,5-benzothiazépine [II] : (voir fig. II) où le Noyau A et le Noyau B sont un noyau benzénique substitué ou non, et R3 est H, un (di-alkylamino inférieur)-alkyle inférieur ou un pipérazinyl-alkyle inférieur substitué ou non, ou un sel de ces derniers, avec un rendement élevé et en une seule étape à partir d'un nouveau composé 3-(2-amino-phénylthio substitué ou non)-2-hydroxy-3-phénylpropionamide substitué ou non. Le dit dérivé de la 1,5-benzothiazépine [II] est utile comme intermédiaire pour la préparation de médicaments comme le chlorhydrate de diltiazem.

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