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Organocatalytic Enantioselective Diels–Alder Reaction of 2‐Trifluoroacetamido‐1,3‐dienes with α,β‐Unsaturated Ketones

Xin‐Qi Zhu, Qian Wang, Jieping Zhu

2022Angewandte Chemie International Edition23 citationsDOIOpen Access PDF

Abstract

We report herein the first examples of chiral phosphoric acid-catalyzed enantioselective Diels-Alder reactions between 2-trifluoroacetamido-1,3-dienes 1 and α,β-unsaturated carbonyl compounds 2. Polysubstituted 1-acetamido cyclohexenes 3 were formed in high yields with excellent diastereo- and enantioselectivities. The reaction proceeds through a stepwise process as shown by deuterium labelling experiments. A catalytic enantioselective three-component reaction of 1, 2 and ortho-hydroxybenzhydryl alcohols 4 was subsequently developed furnishing the densely functionalized hexahydroxanthenes 5 in a highly stereoselective manner. This multicomponent reaction generates four chemical bonds with concurrent creation of five contiguous stereocenters.

Topics & Concepts

Enantioselective synthesisStereocenterChemistryDiels–Alder reactionOrganic chemistryStereoselectivityCatalysisPhosphoric acidOrganocatalysisAsymmetric Synthesis and CatalysisSynthetic Organic Chemistry MethodsAdvanced Synthetic Organic Chemistry
Organocatalytic Enantioselective Diels–Alder Reaction of 2‐Trifluoroacetamido‐1,3‐dienes with α,β‐Unsaturated Ketones | Litcius