Methanesulfonic Acid → 3-Hydroxy-2-(4-methoxyphenyl)-2,3-dihydro-1,5-benzothiazepin-4(5H)-one, (2S,3S)-

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Reaction Steps

A mixture of (2S,3S)-3-(2-aminophenylthio)-2-hydroxy-3-(4-methoxyphenyl)propioamide (1.59 g), xylene (8 ml) and methanesulfonic acid (24 ml) is refluxed for 11 hours. The reaction solution is allowed to cool to room temperature with stirring. The precipitated crystals are collected by filtration, washed with cold methanol, and dried at 50° C. to give (2S,3S)-2,3-dihydro-3-hydroxy-2-(4-methoxyphenyl)-1,5-benzothiazepine-4(5H)-one (1.41 g).

Provenance & Evidence