Chemoenzymatic Asymmetric Synthesis of Pyridine-Based α-Fluorinated Secondary Alcohols

Chembiochem. 2021 Dec 2;22(23):3314-3318. doi: 10.1002/cbic.202100392. Epub 2021 Oct 7.

Abstract

Fluoro-substituted and heteroaromatic compounds are valuable intermediates for a variety of applications in pharma- and agrochemistry and synthetic chemistry. This study investigates the chemoenzymatic preparation of chiral alcohols bearing a heteroaromatic ring with an increasing degree of fluorination in α-position. Starting from readily available picoline derivatives prochiral α-halogenated acyl moieties were introduced with excellent selectivity and 64-95 % yield. The formed carbonyl group was subsequently reduced to the corresponding alcohols using the alcohol dehydrogenase from Lactobacillus kefir, yielding an enantiomeric excess of 95->99 % and up to 98 % yield.

Keywords: alcohol; enantioselectivity; enzymes; fluorine; heteroaromatic.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alcohol Dehydrogenase / metabolism*
  • Alcohols / chemistry
  • Alcohols / metabolism*
  • Halogenation
  • Lactobacillus / enzymology*
  • Molecular Structure
  • Pyridines / chemistry
  • Pyridines / metabolism*

Substances

  • Alcohols
  • Pyridines
  • Alcohol Dehydrogenase

Supplementary concepts

  • Lactobacillus kefiri