Efficient synthesis of 3‐sulfonyl‐1,2‐dihydroquinolines via tandem aza‐Michael addition/cyclizations of N‐acyl‐protected 2‐aminobenzaldehyde with vinyl sulfones

Abstract

A mild and effective method for the synthesis of 3‐sulfonyl‐1,2‐dihydroquinolines from N‐acyl‐protected 2‐aminobenzaldehyde with vinyl sulfones has been established. This reaction could rapidly proceed and exhibit different reactivity when employed the vinyl sulfones as nucleophile on aza‐Michael addition/cyclization reaction, allow for the production of 1,2‐DHQs in high yields up to 95%. In addition, the chemical structure of the product was confirmed by x‐ray single‐crystal structure analysis.