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Updated: Jan 30, 2026

Enzymatic Cascade Reactions for the Synthesis of Chiral Amino Alcohols from L-lysine
Published on: February 16, 2018
Asymmetric Iodoaminocyclization for the Synthesis of Chiral 2-Heteroaryl Pyrrolidines
Yangyang Zhong1, Kehan Zhao1, Kewen Zhong1
1Sichuan Research Center for Drug Precision Industrial Technology, West China School of Pharmacy, Sichuan University, Chengdu 610041, China.
Abstract:
An asymmetric iodoaminocyclization strategy catalyzed by (DHQD)2PHAL has been developed for the synthesis of chiral 2-heteroaryl pyrrolidines, including 2-purinyl and 2-indolyl analogues. This method proceeds under mild conditions and affords the target products in high yields (up to 98%) with excellent diastereoselectivity (trans only) and enantioselectivity (up to 98% ee). The approach provides efficient access to azanucleoside-like scaffolds and demonstrates broad functional group tolerance, highlighting its potential for the synthesis of biologically active pyrrolidine derivatives.
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