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Catalytic Asymmetric (3 + 3) Cycloaddition of Oxyallyl Zwitterions with α-Diazomethylphosphonates

Yan Liu, Xian Peng, Rui She, Xin Zhou, Yungui Peng

2021Organic Letters15 citationsDOI

Abstract

The unique structure of oxyallyls represents a significant challenge for their catalytic asymmetric applications. Herein, an unprecedented chiral imidodiphosphoric acid-catalytic enantioselective (3 + 3) cycloaddition between oxyallyl zwitterions generated in situ from α-haloketones and α-diazomethylphosphonates was developed. Pharmaceutically interesting chiral pyridazine-4(1H)-ones were obtained in up to 98% yields with excellent stereoselectivities (up to 99% ee, > 99:1 dr).

Topics & Concepts

CycloadditionEnantioselective synthesisChemistryCatalysisPyridazineCombinatorial chemistryOrganic chemistryCyclopropane Reaction MechanismsSynthesis and Catalytic ReactionsAsymmetric Synthesis and Catalysis
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