NEW MATERIAL:A 1,5-benzothiazepine derivative expressed by formula I (R1 is lower alkyl, lower alkenyl, phenyl-substituted lower alkyl, hydroxymethyl, lower alkanoyloxy-substituted lower alkyl or formyl; R2 is H, lower alkanoyl, phenyl-substituted lower alkyl or benzoyl; R3 is lower alkyl; R4 is H or lower alkyl; A is lower alkylene; ring A is phenyl) or salts thereof.
EXAMPLE: 2-(4-Methoxyphenyl)-2-methyl-3-hydroxy-5-[2-(dimethylamino)ethyl]-2,3- dihydro-1,5-benzothiazepin-4(5H)-one.
USE: Useful as a medicinal agent having hypotensive, cerebral and coronary vasodilator action.
PREPARATION: A compound expressed by formula II and a compound expressed by formula III (X1 is reacted residue) are subjected to condensing reaction to afford the compound expressed by formula I.
NAGAO HIROSHI
MORIMOTO MASAMICHI
KOUNO HARUYUKI
YASUDA KOUSUKE