Diastereodivergent and Enantioselective Organocatalytic Synthesis of Spiro-Fused Coumarins via [4+2] Cycloadditions

通过[4+2]环加成反应实现螺环稠合香豆素的非对映选择性和对映选择性有机催化合成

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Abstract

A highly enantioselective, organocatalytic, diastereodivergent synthesis of spiro-fused coumarin derivatives via trienamine-mediated Diels-Alder reactions with cyclic 2,5-dienones is reported. Using a cinchonidine-based primary amine and either p-methylbenzoic acid or triethylamine enables reversible diastereoselectivity, providing complementary enantioenriched diastereoisomers. The influence of electron-withdrawing groups at C3 of coumarins is delineated, revealing distinct reactivity patterns. Computational studies provide insight into the mechanism and additive-controlled diastereodivergence.

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