NEW MATERIAL:The compound of formula I (R1 is aryl; R2 and R3 are H, alkyl, alkoxy, halogen or together form alkylene containing 1-2 O atoms; R4 is H, acyl or alkoxycarbonyl; R5 and R6 are alkyl; X is O or S) and its salt.
EXAMPLE: (±)-cis-2,3-Dihydro-5-2-(dimethylamino)ethyl]-3-hydroxy-2-(4- methoxyphenyl)-8-phenoxy-1,5-benzothiazepin-4(5H)-one.
USE: A preventive and remedy for circulatory diseases. Charhcterized by the presence of aryloxy group or arylthio group at 8-site. It has extremely strong hypotensive activity with remarkable prolonged action.
PREPARATION: A compound of formula I wherein R4 is H can be produced e.g. by using a compound of formula II and an epoxy compound of formula III (R7 is alkyl) as starting raw materials and reacting a compound of formula IV derived from the raw materials with a compound of formula V (Y is halogen or sulfonyloxy).
FUJIMOTO KOICHI
SHIMOJI YASUO
KANEZAKI TAKUO
KOIKE HIROYUKI
NISHINO HIROSHI
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