| 摘要 |
PURPOSE:To produce the titled compound easily in high yield, by reacting a specific 1,5-benzothiazepine derivative with dimethylaminoethyl chloride using a catalyst comprising a fluoride supported by cellite, thereby alkylating the 5-N atom of the derivative. CONSTITUTION:The objective compound of formula II is produced either by condensing the 1,5-benzothiazepine derivative of formula I (Ar is phenyl substituted with lower alkoxy; R is lower alkyl) with dimethylaminoethyl chloride in an aprotic polar solvent preferably acetonitrile, etc. at room temperature in the presence of a catalyst comprising a fluoride, preferably tetraalkylammonium fluoride, etc. supported on cellite (the first method) or by reacting the compound of formula I with dimethylaminoethanol in an aprotic polar solvent in the presence of diethylazodicarboxylate using a reducing agent such as triphenyl phosphine, under ice cooling (the second method). The latter method gives higher yield than the first method.
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