PURPOSE: To obtain the titled compound useful as an antithrobotic drug, by condensing a benzothiazepine derivative with a dialkylaminoethyl halogenide.
CONSTITUTION: A benzothiazepine derivative shown by the formula I (R1 is lower lakyl) is condensed with a compound shown by the formula II (R2 and R3 are lower alkyl; X is halogen), and, if necessary, the condensation product is converted into an acid addition salt, to give the desired compound shown by the formula III or its acid addition salt. The reaction is carried out in a proper solvent in the presence of a base (e.g. NaOH) at 0W100°C, preferably at 20W70°C. The compound shown by the formula II can be obtained by hydrolyzing a novel benzothiazepine derivative shown by the formula IV (R4 is lower aklanoyl). The compound shown by the formula IV can be obtained by reacting a compound shown by the formula V with a reactive derivative of a carboxylic acid shown by the formula R4OH in the presence of a compound shown by the formula (R5)2RO(R5 is lower alkyl).
INOUE HIROZUMI
MORITA TAKASHI
ODAWARA AKIO
SASAKI YASUHIKO
Next Patent: BENZOTHIAZEPINE DERIVATIVE AND ITS PREPARATION