Loading patent…
AssigneeAgouron Pharmaceuticals, Inc.
InventorsPei-Pei Kung, Carlos Martinez, Junhua Tao
Estimating the term…
The invention relates to biocatalytic methods for preparing enantiomerically pure stereoisomers of 1-(2,6-dichloro-3-fluorophenyl)ethanol. Disclosed are methods of preparation of the desired (S)-enantiomer, which methods are based on a combination of enzymatic resolution, chemical esterification and chemical hydrolysis with inversion of 1-(2,6-dichloro-3-fluorophenyl)ethyl esters or stereoselective bio-reduction of 2,6-dichloro-3-fluoro-acetophenone with a biocatalyst such as an enzyme or a microorganism. The chiral (S)-enantiomer can be used in the synthesis of certain enantiomerically enriched, ether linked 2-aminopyridine compounds that potently inhibit auto-phosphorylation of human heptocyte growth factor receptor.
(1S)-1-(2,6-dichloro-3-fluorophenyl)ethanol in an enantiomerically pure form.
(1S)-1-(2,6-dichloro-3-fluorophenyl)ethanol having an enantiomeric purity equal to at least 80%.
A composition comprising (1S)-1-(2,6-dichloro-3-fluorophenyl)ethanol substantially free from its corresponding R-enantiomer.
A composition comprising (1S)-1-(2,6-dichloro-3-fluorophenyl)ethanol that is at least 80% free of (1R)-1-(2,6-dichloro-3-fluorophenyl)ethanol.
Dependencies are inferred from the claim text.