ASYMMETRIC FRIEDEL-CRAFTS ALKYLATIONS CATALYZED BY BYFUNCTIONAL CINCHONA ALKALOIDS

摘要

In certain embodiments, the present invention relates to methods for asymmetric Friedel-Craflts alkylation catalyzed by bifunctional cinchona alkaloids. In certain embodiments, the catalyst is a 6'-OH cinchona alkaloid. In certain embodiments, the electrophile is an a-ketoester or aldehyde. In certain embodiments, the nucleophile is an aromatic heterocycle. In certain embodiments, the nucleophile is an aromatic N-containing heterocycle. In certain embodiments, the nucleophile is an indole. In certain embodiments, the methods of the invention are relatively insensitive to concentration, temperature, air and moisture.