Diastereoselective Synthesis of C2'-Fluorinated Nucleoside Analogues Using an Acyclic Approach

J Org Chem. 2016 Nov 18;81(22):10769-10790. doi: 10.1021/acs.joc.6b01845. Epub 2016 Oct 25.

Abstract

Nucleoside analogues bearing a fluorine in the C2'-position have been synthesized by SN2-like cyclizations of acyclic thioaminal precursors. This strategy provides access to two scaffolds, d-1',2'-cis-thiofuranosides and d-1',2'-trans-furanosides, which are difficult to generate using the standard approach for nucleoside synthesis. The addition of silylated nucleobases onto model C2-fluorinated dithioacetal substrates resulted in 1,2-syn diastereoselectivity, which is consistent with the C2-F and S-alkyl moiety being in close proximity. A new series of analogues bearing a C3' all-carbon quaternary center along with a C2'-F atom have also been synthesized using this approach and are being investigated as potential antimetabolites.

Publication types

  • Research Support, Non-U.S. Gov't