One-Pot Synthesis of 1,2-Disubstituted Indoles from 2-Ethynylanilines and Benzaldehydes

An efficient synthesis of a variety of 1,2-disubstituted indoles from 2-ethynylanilines was developed. Using 2-ethynylanilines and benzaldehydes as starting materials, the target products (1,2-disubstituted indoles) were obtained smoothly through condensation, reduction, and subsequent cyclization. Various functional groups attached to the aryl ring of 1,2-disubstituted indoles were well tolerated. The protocol features easy performance, easily available starting materials, good yield, and a broad substrate scope, showing potential synthetic value for the preparation of a variety of biologically or pharmaceutically active compounds.

Automated summary

An efficient synthesis method for 1,2-disubstituted indoles has been developed, providing a straightforward route to the target products from easily accessible starting materials. The protocol offers easy performance, high yield, and a broad substrate scope, indicating its potential synthetic value in the preparation of various biologically or pharmaceutically active compounds.