Experimental study demonstrates room-temperature, regioselective C2-acylation of indoles using dual catalysis, highlighting an efficient route to synthesize bioactive tubulin inhibitors.
A highly regioselective direct C2-acylation of N-pyrimidine protected indoles with aldehydes is reported at room temperature through the merger of visible light photoredox and palladium(ii) catalysis. Late-stage acylation of tryptophan, selective mono-acylation of carbazole and the syntheses of tubulin inhibitors D-64131 and D-68144 are also demonstrated.
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Manna et al. (2017) studied this question.
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