Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1348732 | Tetrahedron: Asymmetry | 2010 | 5 Pages |
Abstract
An efficient four-step biotransformation-mediated synthesis of (1S)-1-(2,6-dichloro-3-fluorophenyl)ethanol in enantiomerically pure form is described. This compound is a key intermediate required for the preparation of PF-2341066, a potent inhibitor of c-Met/ALK that is currently in clinical development. The described synthesis was used to manufacture 6 kg of the title compound and can also be employed to produce the corresponding (1R)-enantiomer.
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(1S)-1-(2,6-Dichloro-3-fluorophenyl)ethanolC8H7Cl2FOEe = 98%αD20=+6.9±1.1 (c 0.87, MeOH)Source of chirality: pig liver esterase
Related Topics
Physical Sciences and Engineering
Chemistry
Inorganic Chemistry
Authors
Carlos A. Martinez, Eric Keller, Renzo Meijer, Gerard Metselaar, Gerlof Kruithof, Curtis Moore, Pei-Pei Kung,