Three-Component Synthesis of α-Aminoperoxides Using Primary and Secondary Dialkylzinc Reagents with O2 and α-Amido Sulfones

Org Lett. 2020 Jul 17;22(14):5380-5384. doi: 10.1021/acs.orglett.0c01692. Epub 2020 Jun 25.

Abstract

A straightforward strategy for the synthesis of unprecedented α-aminoperoxides bearing primary and secondary alkylperoxide substituents is described. Commercially available dialkylzinc reagents are oxidized with molecular oxygen and the consequent peroxide species react with stable (hetero)aromatic and aliphatic α-amido sulfones in excellent yields (>90%). The now available α-aminoperoxides are of potential interest in medicinal chemistry, specifically for the synthesis of antimalarial compounds. Moreover, modification of the reaction conditions selectively leads to N,O-acetals in good yields.

Publication types

  • Research Support, Non-U.S. Gov't