| 摘要 |
NEW MATERIAL:A compound expressed by formula I (R<1> is H or lower alkanoly R<2> and R<3> are lower alkyl; either one of R<4> and R<5> is H, and the other is F) or an acid addition salt thereof. EXAMPLE:( + or - )-cis-2-( 4-Methoxyphenyl )-3-acetoxy-5-[2-( dimethylamino )ethyl]-8- fluoro-2,3-dihydro-1,5-benzothiazepin-4(5H)-one. USE:A medicine, having hypotensive or cerebral or coronary vasodilator action or inhibitory action on blood platelet agglutination with low toxicity, and useful for preventing agent, ameliorant or remedy for cerebral diseases, e.g. hypertension, cerebral angiospasm, cerebral infarction, apoplexy, etc. and cardiopathy, e.g. angina pectoris, arrhythmia, cardiac infarction, etc. PREPARATION:A novel 1,5-benzothiazepine derivative expressed by formula IIor a salt thereof is reacted with a compound expressed by formula III (X is halogen) or a salt thereof in a solvent, preferably in the presence of an alkali reagent to afford the aimed compound expressed by formula I .
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