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Updated: Jul 6, 2026

A Microwave-Assisted Direct Heteroarylation of Ketones Using Transition Metal Catalysis
Published on: February 16, 2020
Asymmetric direct aldol reaction of functionalized ketones catalyzed by amine organocatalysts based on bispidine
Jie Liu1, Zhigang Yang, Zhen Wang
1Key Laboratory of Green Chemistry & Technology, College of Chemistry, Sichuan University, Chengdu 610064, PR China.
Abstract:
Organocatalysts containing primary-secondary amine based on bispidine and amino acid have been designed to catalyze the asymmetric direct aldol reaction of functionalized ketones including alpha-keto phosphonates, alpha-keto esters, as well as alpha,alpha-dialkoxy ketones as aldol reaction acceptors. The corresponding products with chiral tertiary alcohols were obtained in moderate to high yields (up to 97%) and high enantioselectivities (up to 98% ee). A theoretical study of transition structures demonstrated that protonated piperidine was important for the reactivity and enantioselectivity of this reaction.
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