132748-48-2Relevant academic research and scientific papers
Process for preparing 2-aryl-3-hydroxy-cis-2,3-dihydro-1,5-benzothiazepin-4(5H)-ones and their derivatives
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, (2008/06/13)
The present invention relates to a novel process for synthetizing 2-aryl-3-hydroxy-cis-2,3-dihydro-1,5-benzothiazepin-4(5H)-ones and their derivatives, an optically pure compounds or as their racemic mixtures, having the following general formula (I): STR1 by using, as synthesis precursors, methyl esters of 2-hydroxy-3-arylthio-3-arylpropionic acids in their threo form, as their hydrochlorides, or as free bases, of generally formula (II): STR2 and treating such precursors with an excess of sodium methoxide, at low temperature, in diethyleneglycol, dimethylether, diemthylformamide and ethyl acetate.
Method of preparing benzothiazepine derivatives
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, (2008/06/13)
A benzothiazepine derivative of the formula: STR1 wherein R is hydrogen or acetyl, is prepared by condensing a compound of the formula: STR2 wherein R is the same as defined above, with 2-(diamethylamino)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.
