Multistep One-pot Synthesis Of Enantioenriched Polysubstituted Cyclopenta[B] In Doles

We rationally designed a one-pot three-step reaction, including a primary-amine-thiourea catalyzed α-alkylation of aldehydes and two consecutive Bronsted-acid catalyzed Friedel-Crafts reactions[2], to construct chiral polysubstituted cyclopenta[b]indoles. In the promotion of combined chiral amine-thiourea and Bronsted acid catalysts, various3-indoylmethonols, aldehydes and substituted indoles could participate in this reaction and give the target compounds with up to85%yield,99%enantioselectivity and99:1diastereoselectivity.