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Short Paper | Regular issue | Vol 96, No. 2, 2018, pp.324-333
Published online, 24th January, 2018
DOI: 10.3987/COM-17-13857
Synthesis of 2,3-Disubstituted Indoles by Alkylative and Arylative Cyclization of 2-Alkenylphenylisocyanides with Grignard Reagents

Kazuo Yamazaki,* Yasutaka Tajima, Hitomi Tada, Yasuhito Kobayashi, Yutaro Miyamoto, Tomoko Ohkubo, and Masashi Ohba

*Department of Pharmacy, Yokohama University of Pharmacy, 601 Matano-cho, Totsuka-ku, Yokohama 245-0066, Japan


Alkylative cyclization of 3-(2-isocyanophenyl)propenoic acid tert-butyl ester with Grignard reagents proceeds smoothly to form 2-alkylindole-3-acetic acid derivatives in moderate-to-good yields. Substituted 3-(2-isocyanophenyl)propenoic acid tert-butyl esters undergo a similar reaction when phenylmagnesium bromide is used to render 2-phenylindole-3-acetic acid derivatives in moderate-to-good yields.