Processes for the preparation of key intermediate for the synthesis of rosuvastatin or pharmaceutically acceptable salts thereof

摘要

The present invention relates in general to the field of organic chemistry and in particular to a process for the preparation of 5-((E)-2-((2S,4R)-4-hydroxy-6-oxotetrahydro-2H-pyran-2-yl)vinyl)-4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethanesulfonylamino)pyrimidine (RSVL) as well as a process for preparing crystalline 5-((E)-2-((2S,4R)-4-(tert-butyldimethylsilyloxy)-6-oxotetrahydro-2H-pyran-2-yl)vinyl)-4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethanesulfonylamino)pyrimidine (RSVLTBS) useful as key intermediates for the preparation of rosuvastatin or pharmaceutically acceptable salts thereof.

主权项

1. A process for preparing the compound of formula RSVL comprising the steps of:
providing a compound of formula RSVLTBS: converting the compound of formula RSVLTBS into the compound of formula RSVL by removal of silyl protection group in the presence of tetrabutyl ammonium fluoride and acid in organic solvent, and isolating said compound of formula RSVL, further purifying RSVL by extraction with methyl t-butyl ether and forming crystallized RSVL; and recrystallizing the crystallized RSVL using a solvent selected from a group consisting of ethanol, 2-propanol and ethyl acetate and forming recrystallized RSVL.