| 摘要 |
NEW MATERIAL:The compound of formula 1 (Ar is phenyl wherein at least one H is substituted with lower alkoxy; R1 is H or acetyl; R2 is lower alkylene; X is halogen) and its salt. EXAMPLE:2-( 4-Methoxyphenyl )-3-acetoxy-5-( 2-chloroethyl )-2,3-dihydro-1,5-benzothiazepin-4(5H)-one. USE:Useful as a synthetic intermediate of the compound of formula 2 (R3 and R4 are lower alkyl) having coronary vasodilating and psychoneurotic activities, etc. and useful as an excellent drug, and its salt. It can be prepared in high yield and purity. PREPARATION:The compound of formula 1 can be prepared by reacting the compound of formula 3 with the compound of formula 4 (Z is halogen) in an aprotic solvent in the presence of a base such as NaOH, at -5-+50 deg.C.
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