Modular and Chemoselective Strategy for the Direct Access to α-Fluoroepoxides and Aziridines via the Addition of Fluoroiodomethyllithium to Carbonyl-Like Compounds

Org Lett. 2019 Jan 18;21(2):584-588. doi: 10.1021/acs.orglett.8b04001. Epub 2019 Jan 2.

Abstract

An expeditious, high-yielding synthesis of rare α-fluoroepoxides and α-fluoroaziridines through the addition of the unkown fluoroiodomethyllithium (LiCHIF)-formed via deprotonation the commercially available fluoroiodomethane with a lithium amide base-to carbonyl-like compounds is documented. The ring-closure reactions, leading to α-fluorinated three-membered heterocycles, rely on the diversely reactive C-I and C-F bonds. Excellent chemoselectivity was observed in the presence of highly sensitive functionalities-aldehyde, ketone, nitrile, alkene-which remained untouched during the homologation sequence.

Publication types

  • Research Support, Non-U.S. Gov't