NEW MATERIAL:A 2-phenyl [or 2-(4-substituted phenyl)]-2-hydro-5-substituted-1,5- benzothiazepine-3,4(5H)-dione shown by the formula I (R1 is H, halogen, or lower alkoxy; R2 is lower alkyl, lower alkoxyalkyl, lower alkyl which may be replaced with hydroxyl group or halogen, or lower dialkylaminoalkyl) or its acid addition salt.
EXAMPLE: 2-Phenyl-2-hydro-5-methyl-1,5-benzothiazepine-3,4-(5H)-dione.
USE: Useful as a drug having vasodilating action on coronary blood vessel, antiarrhythmic action, analgesic action, inhibitory action on blood platelet aggregation, etc. Also useful as an intermediate for synthesizing a remedy for angina of effort as a vasodilator for coronary blood vessel, angina pectoris in myocardial infarction inveterata, etc.
PROCESS: A compound shown by the formula II is reacted with hydrogen peroxide and a trimethylhalogenosilane, to give a compound shown by the formula III(X is halogen), which is subjected to ring enlargement, to give a compound shown by the formula I .
MAEDA SADAYUKI
UNEDA TAKASHI
TAKATANI MASAHIRO
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