Asymmetric Iodoaminocyclization for the Synthesis of Chiral 2-Heteroaryl Pyrrolidines

Organic Letters 2026

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Authors: Yangyang Zhong, Kehan Zhao, Kewen Zhong, Tianlan Zhao, Hongping Zhu, Huijing Wang, Fener Chen
DOI: 10.1021/acs.orglett.5c05072
Cited by: 1
References: 41

Abstract

An asymmetric iodoaminocyclization strategy catalyzed by (DHQD) 2 PHAL 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.

Fields of Study & Subjects

Catalytic C–H Functionalization Methods Vanadium and Halogenation Chemistry Catalytic Alkyne Reactions

Publication details

Journal / source
Organic Letters
Publisher
American Chemical Society (ACS)
Volume
28
Issue
6
Pages
1964–1969
Publication date
29 January 2026
Language
EN