PROCESS FOR THE PREPARATION OF (2S,3S)-3-ACETOXY-5-(N, N-DIMETHYLAMINOETHYL)-2-(4-METHOXYPHENYL)-2,3-DIHYDRO- 1,5-BENZOTHIAZEPIN-4(5H)-ONE

摘要

PROCESS FOR THE PREPARATION OF /2S,3S/-3-ACETOXY-5- -/N,N-DIMETHYLAMINOETHYL/-2-/4-METHOXYPHENYL/-2,3- -DIHYDRO-1,5-BENZOTHIAZEPIN-4/5H/-ONE A b s t r a c t The invention relates to a new process for the preparation of /2S,3S/-3-acetoxy-5-/N,N-dimethyl-aminoethyl/-2-/4-methoxyphenyl/-2,3-dihydro-1,5-benzo-thiazepin-4/5H/-one of the formula /I/ (1) and acid addition salts thereof, by a/ alkylation and acetylation of /2S,3S/-3- -hydroxy-2-/4-methoxyphenyl/-2,3-dihydro-1,5-benzo-thiazepin-4/5H/-one of the formula /III/ (111) in an optional order, or b/ alkylation of 3-acetoxy-2-/4-methoxyphenyl/- -2,3-dihydro-1,5-benzothiazepin-4/5H/-one of the formula /V/ (V) and if desired, conversion of the compound of formula /I/ obtained into an acid addition salt thereof, w h i c h c o m p r i s e s carrying out the alkylation with 2-dimethylaminûethanol mesylate hydrochloride and/or carrying out the acetylation with isopropenyl acetate.