A NOVEL PROCESS FOR THE PREPARATION OF (2S,3R,4R,5S,6R)-2-{3-5-4-FLUORO- PHENYL)-THIOPHEN-2-YLMETHYL-4-METHYL-PHENYL}-6-HYDROXYMETHYL-TETRAHYDRO-PYRAN-3,4,5-TRIOL AND ITS STABLE AMORPHOUS HEMIHYDRATE FORM

摘要

The present invention discloses the process for preparation of (2S,3R,4R,5S,6R)-2-{3-[5-[4-Fluoro-phenyl)-thiophen-2-ylmethyl]-4- methyl-phenyl}-6-hydroxymethyl-tetrahydro-pyran-3,4,5-triol and its pipecolic acid co-crystal. The invention also discloses novel intermediate, acetic acid 4, 5-diacetoxy-6-acetoxymethyl-2-R1-2-{3-[5-(4-fluoro-phenyl)-thiophen-2-ylmethyl]-4-methyl-phenyl}- tetrahydro-pyran-3-yl ester, wherein, R1 is allyl or prop-2-ynyl, as an intermediate for the preparation of 4, 5-diacetoxy-6- acetoxymethyl-2-R1-2-{3-[5-(4-fluoro-phenyl)-thiophen-2-ylmethyl]-4-methyl-phenyl}-tetrahydro-pyran-3-yl ester, wherein, R1 is allyl or prop-2-ynyl.