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US 2006/0069137 A1Published application
Novel process for ezetimibe intermediate
AssigneeHetero Drugs Limited
InventorsBandi Parthasaradh Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara, 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
1) 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 R 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
13) A process according to claim 13, wherein about 0.8 to 5 moles of (−)-DIP chloride per mole of the keto compound of formula 3 is used.
Dependencies are inferred from the claim text.