Menetelmä (+)-(2S,3S)-3-hydroksi-2-(4-metoksifenyyli)-2,3-dihydro-5H-1,5-bentsotiatsepiini-4-onin ja sen kloorattujen johdannaisten valmistamiseksi

摘要

The invention relates to a process for preparing (+) (2S,3S)-3-hydroxy-2-(4-methoxyphenyl)-2,3-dihydro-5H-1,5 benzothiazepin-4-one, whose aromatic ring optionally includes a chlorine atom, by reacting 2-aminothiophenol with methyl (-)- (2R,3S)-2,3-epoxy-3-(4 methoxyphenyl)propionate, after which the methyl(2S,3S)-3 [(2-aminophenyl)thio]-2-hydroxy-3-(4 methoxyphenyl)propionate is cyclised in the presence of methanesulphonic acid, in the same vessel without isolating the said intermediate, using a chlorinated hydrocarbon whose boiling point exceeds 70 degree C as a solvent. These compounds are useful pharmaceutical intermediates.