Process for preparing optically active benzothiazepine...

Details Process for preparing optically active benzothiazepine... Process for preparing optically active benzothiazepine...

C - Chemistry, Metallurgy

07

D

C07D 281/10 (2006.01)

Patent

CA 2086862

29 ABSTRACT OF THE DISCLOSURE: Process for preparing optically active cis-3-hydroxy- 2,3-dihydro-1,5-benzothiazepin-4(5H)-one compounds [I] of the formula: Image [I] wherein Ring A and Ring B are substituted or unsubstituted benzene, R1 is hydrogen or di-lower alkylaminoalkyl, which comprises subjecting 1,5-benzothiazepin-4(5H)-one (II) of the formula (II): Image [II] wherein R4 is hydrogen or lower alkanoyl, and the other symbols are the same as defined above, to asymmetric reduction with a reaction product of optically active .alpha.-amino acid and metal hydride, in high optically yield, and said compounds [I] are very important as intermediate for preparing various medicines.

Méthode pour préparer des dérivés de cis-3-hydroxy- 2,3-dihydro-1,5- benzothiazépin-4(5H)-one (I) de formule Image - dans laquelle, les cycles A et B sont des benzènes avec ou sans substitution, et R1 est un hydrogène ou un dialkyl(inf.)aminoalkyle -, consistant à soumettre la 1,5-benzothiazépin-4(5H)-one (II) de formule (II) Image - dans laquelle R4 est de l'hydrogène ou un alcanoyle inf., les autres symboles correspondant aux définitions données ci-dessus - à une réduction asymétrique avec un produit de réaction d'un acide alpha-aminé optiquement actif et d'un hydrure de métal, donnant un rendement optiquement élevé; les composés (I) sont très importants comme intermédiaires pour la préparation de médicaments.

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