One-Pot Synthesis of Indole-3-acetic Acid Derivatives through the Cascade Tsuji–Trost Reaction and Heck Coupling

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A practical palladium-mediated cascade Tsuji–Trost reaction/Heck coupling of N-Ts o -bromoanilines with 4-acetoxy-2-butenonic acid derivatives using a Pd(OAc) 2 /P( o -tol) 3 /DIPEA system is described for a straightforward synthesis of indole-3-acetic acid derivatives. This methodology was successfully applied to synthesize various substituted indole/azaindole-3-acetic acid derivatives and Almotriptan, which is a drug for the acute treatment of migraines. Moreover, a plausible cyclization mechanism has been proposed.