F.i.s. Fabbrica Italiana Sintetici S.p.a.

Amleto Rizzi

Gaetano Marchioro

The present invention relates to a process for the separation of the enantiomers of threo-2-hydroxy-3-(2'- aminophenylthio)-3-(4'-methoxyphenyl)-propionic acid, which is an important intermediate in the synthesis of pharmacologically active compounds, by means of the direct crystallization of the relevant cyclohexylaminic salt. According to a preferred form of practical embodiment of the present invention, the optically pure acid is recovered as the hydrochloride of the corresponding methyl ester.

Process for the optical resolution of

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.

Growing community of inventors

Alte Ceccato, Italy

Amleto Rizzi