Enzymatic process for the preparation of (S)-5-(4-fluoro-phenyl)-5-hydroxy-1morpholin-4-yl-pentan-1-one, an intermediate of Ezetimibe and further conversion to Ezetimibe
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United States of America Patent
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Jul 12, 2016
Issued Date -
N/A
app pub date -
Mar 30, 2010
filing date -
Apr 1, 2009
priority date (Note) -
In Force
status (Latency Note)
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Abstract
The present invention provides an enzymatic process for the preparation of (S)-5-(4-Fluoro-phenyl)-5-hydroxy-1morpholin-4-yl-pentan-1-one by the reduction of 1-(4-Fluoro-phenyl)-5-morpholin-4-yl-pentane-1,5-dione by using a suitable enzyme or by the resolution of (R,S)-5-(4-Fluoro-phenyl)-5-hydroxy-1morpholin-4-yl-pentan-1-one by using an enzyme. The present invention also provides process for the preparation of Ezetimibe comprising the steps of a) protecting the compound (S)-5-(4-Fluoro-phenyl)-5-hydroxy-1morpholin-4-yl-pentan-1-one with hydroxy protecting group b) hydrolyzing the obtained compound c) condensing with a chiral auxiliary d) reacting with an protected imine compound e) converting to alkyl ester f) cyclizing and g) deprotecting to obtain Ezetimibe.
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International Classification(s)
- 2010 Application Filing Year
- C12P Class
- 1859 Applications Filed
- 1029 Patents Issued To-Date
- 55.36 % Issued To-Date
Cited Art Landscape
Patent Citation Ranking
- 0 Citation Count
- C12P Class
- 0 % this patent is cited more than
- 9 Age
Maintenance Fees
| Fee | Large entity fee | small entity fee | micro entity fee | due date |
|---|---|---|---|---|
| 11.5 Year Payment | $7400.00 | $3700.00 | $1850.00 | Jan 12, 2028 |
