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US 7,067,675 B2Granted
Process for ezetimibe intermediate
AssigneeHetero Drugs Limited
InventorsBandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Kesireddy Subash Chander Reddy
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Abstract
The invention provides a process for preparing intermediate of ezetimibe, which shows hypocholesterolemic activity. Thus 3-[5-(4-fluorophenyl)-1,5-dioxopentyl]-4-phenyl-2-oxazolidinone is reduced with (−)-DIP chloride to obtain 3-[(5S)-5-(4-fluorophenyl)-5-hydroxy-1-oxopentyl]-4-phenyl-2-oxazolidinone.
Claims13
A process for the preparation of an alcohol of formula 2:
- wherein X is O or S;
- Y is O, S or N(lower alkyl);
- and R1 is alkyl, unsubstituted or substituted phenyl, unsubstituted or substituted naphthyl or lower alkoxy carbonyl, wherein substituents on phenyl and naphthyl are selected from the group consisting of lower alkyl and phenyl;
- which comprises reducing the ketone of formula 3:
- wherein X—, Y— and R1 are as defined above, with (−)-DIP chloride ((−)-β-chlorodiisopinocampheylborane).
2 more elements
Dependencies are inferred from the claim text.