One-Pot Synthesis of 2-Styrylindoles from Ortho -Substituted Chloroenynes

Guangkuan Zhao (1) , Jérôme Bignon (2) , Hélène Lévaique (2) , Joëlle Dubois (2) , Mouad Alami (1) , Olivier Provot (1)

1 BioCIS - Biomolécules : Conception, Isolement, Synthèse
2 ICSN - Institut de Chimie des Substances Naturelles

A facile one pot synthesis of 2-styrylindoles, through Suzuki-arylation of ortho-substituted chloroenynes followed by N-cyclization and N-demethylation has been developed. A variety of 2-styrylindoles were obtained in good to excellent yields and were evaluated for their anticancer properties.

Mots clés: 2-Styrylindole; palladium; Suzuki; coupling; cyclization

Domaines: Chimie organique

Guangkuan Zhao, Jérôme Bignon, Hélène Lévaique, Joëlle Dubois, Mouad Alami, et al.. One-Pot Synthesis of 2-Styrylindoles from Ortho -Substituted Chloroenynes. Journal of Organic Chemistry, 2018, 83 (24), pp.15323-15332. ⟨10.1021/acs.joc.8b02563⟩. ⟨hal-02394175⟩