Novel method of preparing benzothiazepine derivatives.

摘要

A benzothiazepine derivative of the formula:
<Chemistry id="chema01" num="0001"><Image id="ia01" he="36" wi="72" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>wherein R is hydrogen or acetyl, is prepared by condensing a compound of the formula:
<Chemistry id="chema02" num="0002"><Image id="ia02" he="32" wi="77" file="IMGA0002.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>wherein R is the same as defined above, with 2-(dimethylamino)-ethyl halide (i) in the presence of potassium hydroxide in acetone; or (ii) in the presence of potassium carbonate in acetone, lower alkyl acetate, a mixture of acetone and water or a mixture of lower alkyl acetate and water.