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US 8,273,917 B2Granted
Method for preparing chiral baclofen
AssigneeSCI Pharmtech, Inc.
InventorsJen-Huang Kuo, Wei-chyun Wong
Life of this patent
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Abstract
The present invention provides a novel method for preparing chiral Baclofen with higher yield, higher e.e. value, and lower cost via chiral Michael addition.
Claims13
A method for preparing (R)-Baclofen of formula (I),
- comprising the steps of:
- reacting p-chlorocinamic acid with a chiral auxiliary compound of formula II to form a compound of formula III;
- performing Michael addition of nitromethane to a compound of formula III to give a compound of formula IV via diastereomeric selection;
- performing hydrolysis of the compound of formula IV to obtain a compound of formula V and recover the chiral auxiliary compound of formula II;
- and reducing a nitro group of the compound of formula V to yield (R)-Baclofen of formula I,
- wherein R1 and R2 are independently a hydrogen atom, an alkyl group having 1 to 8 carbon atoms or an aryl group having 6 to 10 carbon atoms;
- R3 is an alkyl group having 1 to 8 carbon atoms or an aryl group having 6 to 10 carbon atoms;
- and X is N, O or S.
5 more elements
Dependencies are inferred from the claim text.