Synthesis of tetrahydropyridazines by a metal-carbene-directed enantioselective vinylogous N-H insertion/Lewis acid-catalyzed diastereoselective Mannich addition

通过金属卡宾导向的对映选择性乙烯基NH插入/路易斯酸催化的非对映选择性曼尼希加成反应合成四氢哒嗪。

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Abstract

A versatile cascade of reactions, 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.

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