Diastereoselective construction of spiro-cyclopropyl-pyrazoles via a [2 + 1] annulation reaction of iminoindoline-derived alkenes and 4-bromo-pyrazolones

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Authors: Dan Hu, Heng Yin, Fuyu Li, Jiao He, Chenlong Deng, Lixia Liu, Wen Xia, Yulong Li, Chenyi Li
Cited by: 3
References: 61

Abstract

A base-promoted [2 + 1] annulation reaction between iminoindoline-derived alkenes and 4-bromo-pyrazolones has been disclosed, affording a series of novel, pharmaceutically interesting spiro-cyclopropyl pyrazolones containing indolines in good to excellent yields with moderate to good diastereoselectivities. This protocol features broad functional group compatibility, simple operation, and mild reaction conditions.

Fields of Study & Subjects

Catalytic C–H Functionalization Methods Cyclopropane Reaction Mechanisms Synthesis and Reactivity of Heterocycles

Publication details

Journal / source
Organic & Biomolecular Chemistry
Publisher
Royal Society of Chemistry (RSC)
Volume
24
Issue
5
Pages
1063–1068
Publication date
1 January 2026
Language
EN