Journal
CHEMICAL COMMUNICATIONS
Volume 52, Issue 1, Pages 80-83Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c5cc07880f
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Funding
- NSFC [21402065]
- Shanghai Institute of Technology
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An efficient self-assembled methanoproline-thiourea organocatalyst for the synthesis of optically active 6-isopropyl-3,4-dihydropyrimidines via an asymmetric Biginelli reaction was developed, which is superior to the individual precatalyst. A wide range of optically active 6-isopropyl-3,4-dihydropyrimidines with remarkable pharmacological interest was obtained in high yields with excellent enantioselectivities (up to 99% ee). A plausible transition state has been proposed to explain the origin of the activation and the asymmetric induction.
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