Nippon Kayaku Kabushiki Kaisha

Tanabe Seiyaku Company, Limited

Hidefumi Kinoshita

Katsuhiko Kurabayashi

Toshio Takahashi

Nobuyuki Futamura

Hitoshi Saito

Susumu Nagao

Disclosed herein are a process for producing 4'-demethyl-epipodophyllotoxin-.beta.-D-ethylidene-glucoside of the formula (II) comprising (A) reacting 4'-halogenoacetyl-4'-demethyl-epipodophyllotoxin-.beta.-D-2,3-di-O-halogen oacetyl-4,6-O-ethylidene-glucoside of the formula (I) with an amine and/or ammonia, or (B) subjecting the acyl-derivative (I) to alcoholysis in the presence of a catalyst, thereby removing the halogenoacetyl groups of the acyl-derivative (I) to obtain the compound (II), the acyl-derivative (I), and the use of the acyl-derivative (I) for synthesizing the compound (II) ##STR1## wherein R represents a halogenoacetyl group represented by the formula

Process for producing

A process for preparing 1,5-benzothiazepine derivatives of the formula: ##STR1## wherein Ar is a phenyl substituted with a lower alkoxy, R is a lower alkyl, R.sup.1 and R.sup.2 are each a lower alkyl, and Y is a lower alkylene, which have excellent coronary vasodilating and psychoneurotic activities and are useful particularly as a Ca.sup.++ -antagonistic coronary vasodilator.

Process for preparing 1,5-benzothiazephine derivatives

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Takasaki, Japan

Hidefumi Kinoshita