Synthesis of Tetrahydropyridazines by a Metal-carbene Directed Highly Enantioselective Vinylogous N-H Insertion/Lewis Acid Catalyzed Diastereoselective Mannich Addition

摘要

A versatile reaction cascade triggered by Rh(II)-catalyzed diazo decomposition followed by a vinylogous N-H insertion/Lewis acid catalyzed Mannich addition that produces highly substituted 1,2,3,6-tetrahydropyridazines in up to 97% ee with high yield and diastereocontrol has been developed.