Regioselective synthesis of substituted arenes via aerobic oxidative [3 + 3] benzannulation reactions of α,β-unsaturated aldehydes and ketones

Org Lett. 2015 Mar 20;17(6):1449-52. doi: 10.1021/acs.orglett.5b00318. Epub 2015 Feb 27.

Abstract

Facile conversion of α,β-unsaturated aldehydes and ketones into highly substituted arenes via a base-mediated, completely regioselective, air-oxidative [3 + 3] benzannulation reaction with readily available 4-sulfonylcrotonates or 1,3-bisphenylsulfonylpropene is reported. The reaction can also be carried out as a one-pot, three-component operation using 4-bromocrotonates, aryl sulfinates, and cinnamaldehyde. This open-flask, metal-free reaction does not require anhydrous solvents, proceeds under mild conditions, and uses atmospheric oxygen as the oxidant to afford high yields of the 3-(arylsulfonyl)benzoic acid esters.

Publication types

  • Research Support, Non-U.S. Gov't