PURPOSE: To obtain the titled compound useful as coronary vasodilator, etc. by one stage, by reacting a 1,5-benzothiazepine derivative with an N,N-dialkylaminoalkyl halide by the use of KF-Al2O2 as an alkylation promotor.
CONSTITUTION: A 1,5-benzothiazepine derivative shown by the formula I (A is lower alkoxy; R is lower alkyl) is reacted with an N,N-dialkylaminoalkyl halide shown by the formula II (X is halogen; Y is lower alkylene; R1 and R2 are lower alkyl) in an aprotic solvent such as acetonitrile, or tetrahydrofuran in the presence of KF-Al2O3 to give an N-substituted-1,5-benzothiazepine derivative shown by the formula III or its salt [e.g., d-3-acetoxy-cis-2,3-dihydro-5-[-2-(dimethylamino)ethyl]-2-(para-methoxyphenyl)-1,5-benzothiazepine-4-(5H)-one, etc.] shown by the formula III.
ISHIZUKA YORIYASU
FUTSUKAICHI OSAMU
