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Chemo- and regioselective ethynylation of 4,5,6,7-tetrahydroindoles with ethyl 3-halo-2-propynoates
Authors:Boris A. Trofimov, Lyubov&#x   N. Sobenina, Zinaida V. Stepanova, Ol&#x  ga V. Petrova, Igor&#x   A. Ushakov,Al&#x  bina I. Mikhaleva
Affiliation:

aA. E. Favorsky Irkutsk Institute of Chemistry, Siberian Branch of the Russian Academy of Sciences, 1 Favorsky St., Irkutsk 664033, Russian Federation

Abstract:
4,5,6,7-Tetrahydroindoles undergo a rapid, facile (rt, 60 min) ethynylation with ethyl 3-halo-2-propynoates upon grinding with solid K2CO3 (without solvent) at C-2 of the tetrahydroindole ring to afford ethyl 3-(4,5,6,7-tetrahydroindol-2-yl)-2-propynoates in 62–90% yield.
Keywords:4,5,6,7-Tetrahydroindoles   Indoles   Active surface   K2CO3   Cross-coupling
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