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Biotransformation-mediated synthesis of (1S)-1-(2,6-dichloro-3-fluorophenyl)ethanol in enantiomerically pure form
Tetrahedron: Asymmetry Pub Date : 7 October 2010 , DOI: 10.1016/j.tetasy.2010.09.007
Carlos A. Martinez , Eric Keller , Renzo Meijer , Gerard Metselaar , Gerlof Kruithof , Curtis Moore , Pei-Pei Kung

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.

中文翻译:

对映体纯形式的(1 S)-1-(2,6-二氯-3-氟苯基)乙醇的生物转化介导的合成

描述了一种高效的四步生物转化介导的对映体纯形式的(1 S)-1-(2,6-二氯-3-氟苯基)乙醇的合成。该化合物是制备PF-2341066所需的关键中间体,PF-2341066是目前正在临床开发中的强效c-Met / ALK抑制剂。所描述的合成用于制备6kg的标题化合物,并且还可用于制备相应的(1R)-对映异构体。
更新日期:2017-01-31
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