Biocatalytic Fluoroalkylation Using Fluorinated S-Adenosyl-l-methionine Cofactors

Org Lett. 2023 Aug 4;25(30):5650-5655. doi: 10.1021/acs.orglett.3c02028. Epub 2023 Jul 25.

Abstract

Modification of organic molecules with fluorine functionalities offers a critical approach to develop new pharmaceuticals. Here, we report a multienzyme strategy for biocatalytic fluoroalkylation using S-adenosyl-l-methionine (SAM)-dependent methyltransferases (MTs) and fluorinated SAM cofactors prepared from ATP and fluorinated l-methionine analogues by an engineered human methionine adenosyltransferase hMAT2AI322A. This work introduces the first example of biocatalytic 3,3-difluoroallylation. Importantly, this strategy can be applied to late-stage site-selective fluoroalkylation of complex molecule vancomycin with conversions up to 99%.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Biocatalysis
  • Humans
  • Methionine* / metabolism
  • Methyltransferases / metabolism
  • Racemethionine
  • S-Adenosylmethionine* / metabolism

Substances

  • Methionine
  • S-Adenosylmethionine
  • Methyltransferases
  • Racemethionine