| 摘要 |
Production of 5-aminoalkyl-2-phenyl-3-acyloxy-2,3-dihydro-1,5-benzothiazepin-4(5H)-one derivatives of formula (III) comprises (a) reacting a 2-phenyl-3-hydroxy-2,3-dihydro-1,5-benzothiazepin-4(5H)-one derivative of formula (II) with an aminoalkylating agent in the presence of an alkali metal carbonate and a solvent that forms hydrogen bonds with (II) to produce a 5-aminoalkyl-2-phenyl-3-hydroxy-2,3-dihydro-1,5-benzothiazepin-4(5H)-one derivative of formula (I) and (b) reacting (I) with an acylating agent in the presence of a basic catalyst. R1 = (CH2)nNR3R4; n = 1-4; R3, R4 = 1-10C alkyl, aryl, alkaryl or aralkyl; R2 = H, OH or 1-6C alkoxy; R5 = 1-10C alkyl, aryl, alkaryl or aralkyl. Also claimed is the production of (I) by step (a) per se. Aminoalkylation is preferably effected with R1X, where X = Cl, Br or I (especially Cl), in the presence of potassium carbonate and a ketone, ester, ether, alcohol or O- or N-containing heterocyclic solvent, especially MIBK, at reflux temperature. Acylation is effected with R5COCl or (R5CO)2O, especially acetic anhydride, at reflux temperature.
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