| 摘要 |
NEW MATERIAL:The 8-chloro-1,5-benzothiazepine derivative of formula I (R<1> is H, lower alkyl, etc.; R<2> and R<3> are lower alkyl) or its acid addition salt. EXAMPLE:(+)-Cis-2-(4-Methoxyphenyl)-3-acetoxy-5-[2-(dimethylam-in-o)-e thyl]-8- chloro-2,3-dihydro-1,5-benzothiazepin-4(5H)-one hydro-chloride. USE:A hypotensor and cerebral and coronary vasodilator. It has higher activity than 7-chloro-1,5-benzothiazepine derivative, and has low side effect and toxicity. PREPARATION:The compound of formula I wherein R<1> is H can be prepared by the condensation reaction of the compound of formula II (R<5> is H) or its salt with the compound of formula III (X is halogen) or its salt in a solvent (e.g. acetone, ethyl acetate, etc.) at 0-100 deg.C.
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