Practical One‐Pot Procedure for the Synthesis of 1,2,3,4‐Tetrahydroquinolines by the Imino‐Diels‐Alder Reaction

Abstract

A novel‐one‐pot procedure for the synthesis of tetrahydroquinolines via the imino‐Diels‐Alder reaction is described. This procedure gives better yields and exhibits better versatility for alkene substrates than the existing hemi‐aminal based methodologies.

Keywords:

• Imino‐Diels‐Alder reaction
• one‐pot procedure
• tetrahydroquino lines

Acknowledgments

The authors want to thank Tarek Mansour and Semiramis Ayral‐Kaloustian for overseeing the Wyeth summer intern program and for their constant support and encouragement. Further thanks belong to the discovery analytical chemistry (DAC) group at Wyeth, Pearl River, for analytical support, and my laboratory coworkers Zecheng Chen and Oswaldo DosSantos for their help in the laboratory.