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Synthesis of Indole‐Fused Eight‐Membered Oxa‐Rings via Palladium‐Catalyzed Asymmetric [4+4] Cycloaddition of Indole‐2,3‐Quinodimethanes with 2‐Alkylidenetrimethylene Carbonates

Xinhao Lu, Yi-Xiang Wang, Chenghan He, Yang‐Zi Liu, Wei‐Ping Deng

2024Chinese Journal of Chemistry18 citationsDOIOpen Access PDF

Abstract

Comprehensive Summary We report a palladium‐catalyzed asymmetric [4+4] cycloaddition reaction between 2‐alkylidenetrimethylene carbonate and electron‐deficient indole‐2,3‐quinodimethanes ( IQDMs ). This reaction features exclusive regioselectivity, high yield (up to 98%), excellent enantioselectivity (up to 95% ee), and easy scale‐up without any loss of efficiency, making it valuable for the synthesis of indole‐fused eight‐membered oxa‐rings.

Topics & Concepts

ChemistryIndole testCycloadditionCatalysisPalladiumCombinatorial chemistryMedicinal chemistryStereochemistryOrganic chemistryCatalytic Alkyne ReactionsSynthesis of Indole DerivativesOxidative Organic Chemistry Reactions
Synthesis of Indole‐Fused Eight‐Membered Oxa‐Rings via Palladium‐Catalyzed Asymmetric [4+4] Cycloaddition of Indole‐2,3‐Quinodimethanes with 2‐Alkylidenetrimethylene Carbonates | Litcius