Synthesis of 2-fluoro-2-pyrrolines via tandem reaction of α-trifluoromethyl-α,β-unsaturated carbonyl compounds with N-tosylated 2-aminomalonates

Chem Commun (Camb). 2016 Apr 7;52(27):4922-5. doi: 10.1039/c6cc00831c. Epub 2016 Mar 15.

Abstract

A simple base-mediated tandem SN2'/SNV reaction of the readily available α-trifluoromethyl-α,β-unsaturated carbonyl compounds with N-tosylated 2-aminomalonates was developed, which provide an efficient access to functionalized tetrasubstituted 2-fluoro-2-pyrrolines in good to excellent yields. In contrast, simple 1,2-nucleophilic adducts were produced when α-trifluoromethyl styrenes were used.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Ketones / chemistry*
  • Malonates / chemistry*
  • Pyrroles / chemical synthesis*

Substances

  • Ketones
  • Malonates
  • Pyrroles
  • pyrroline
  • malonic acid