Asymmetric Synthesis of Pyrrolidines via Oxetane Desymmetrization

Org Lett. 2022 Apr 1;24(12):2359-2364. doi: 10.1021/acs.orglett.2c00564. Epub 2022 Mar 24.

Abstract

Asymmetric synthesis of chiral pyrrolidines bearing an all-carbon quaternary stereocenter in the 3-position remains challenging. Herein we report two efficient protocols by means of oxetane desymmetrization, featuring the use of a readily available tert-butylsulfinamide chiral auxiliary and a catalytic system with chiral phosphoric acid as the source of chirality, respectively.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Catalysis
  • Ethers, Cyclic*
  • Pyrrolidines*
  • Stereoisomerism

Substances

  • Ethers, Cyclic
  • Pyrrolidines
  • oxetane