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■ An Effective Method for Formylation of Weakly Nucleophilic Anilines and Indole

Isamu Shiina, Mitsutomo Miyashita, Masashi Nagai, and Teruaki Mukaiyama

*Department of Applied Chemistry, Faculty of Science, Science University of Tokyo, Kagurazaka 1-3, Shinjuku-ku, Tokyo 162-8601, Japan

Abstract

In the presence of a catalytic amount of active titanium(IV) salt or Yb(OTf)₃, weakly nucleophilic anilines and indole react under mild conditions with formic acid or aqueous formic acid to afford respectively the corresponding formanilides and indole-3-carboxaldehyde in excellent yields using 4-trifluoromethylbenzoic anhydride as a coreagent.