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

Abstract

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

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Article information

Article type
Paper
Submitted
21 Nov 2025
Accepted
02 Jan 2026
First published
06 Jan 2026

Org. Biomol. Chem., 2025, Accepted Manuscript

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

D. Hu, H. Yin, F. Li, J. He, C. Deng, L. Liu, W. Xia, Y. Li and C. Li, Org. Biomol. Chem., 2025, Accepted Manuscript , DOI: 10.1039/D5OB01841B

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