Diltiazem prodn. from 5-unsubstituted 3-hydroxy analogue

Prodn. of (25,35)-3-acetoxy-5-(N,N-dimethyl aminoethyl)-2-(4- methoxyphenyl)-2,3-dihydro -1,5-benzothiazepin-4(5H)-one (I), or its acid addn. salts, comprises (1) alkylation and acetylation, in either order, of the hydroxy cpd. (III) or (2) alkylation of the 3-acetoxy cpd. (V). The new features are that alkylation is with 2-dimethylaminoethanol mesylate hydrochloride (A) and/or acetylation is with isopropenyl acetate (B). Prodn. of (25,35)-3-acetoxy-5-(N,N-dimethyl aminoethyl)-2-(4- methoxyphenyl)-2,3-dihydro -1,5-benzothiazepin-4(5H)-one (I), or its acid addn. salts, comprises (1) alkylation and acetylation, in either order, of the hydroxy cpd. (III) or (2) alkylation of the 3-acetoxy cpd. (V). The new features are that alkylation is with 2-dimethylaminoethanol mesylate hydrochloride (A) and/or acetylation is with isopropenyl acetate (B). (Machine-translation by Google Translate, not legally binding) PROCEDIMIENTO DE PREPARAR DERIVADOS BENZOTIACEPIN-4(5H)-ONICOS, PARTICULARMENTE DERIVADOS DE LA FORMULA GENERAL (I) Y SUS SALES DE ADICION DE ACIDO, MEDIANTE ALQUILIZACION Y ACETILACION DE (2S,3S)-3-HIDROXI-2-(4-METOXIFENIL)-2,3-DIHIDRO-1,5-BENZOTIACEPIN-4(5H)-ONA O ALQUILIZACION DE 3-ACETOXI-2-(4-METOXIFENIL)-2,3-DIHIDRO-1,5-BENZOTIACEPIN-4(5H)-ONA, QUE COMPRENDE REALIZAR LA ALQUILIZACION CON CLORHIDRATO DE MESILATO DE 2-DIMETILAMINOETANOL Y/O REALIZAR LA ACETILACION CON ACETATO DE ISOPROPENILO. LOS COMPUESTOS OBTENIDOS TIENEN ACTIVIDAD ANTAGONISTA DE CALCIO Y EL PROCEDIMIENTO PERMITE OBTENERLOS CON RENDIMIENTO EXCELENTE, EN UN TIEMPO MUY CORTO.