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Updated: Jun 8, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Efficient generation of biologically active H-pyrazolo[5,1-a]isoquinolines via multicomponent reaction
1Department of Chemistry, Fudan University, 220 Handan Road, Shanghai 200433, China.
Abstract:
A highly efficient multicomponent reaction of 2-alkynylbenzaldehyde, sulfonohydrazide, alcohol, and α,β-unsaturated aldehyde or ketone is disclosed, which generates the diverse H-pyrazolo[5,1-a]isoquinolines in good yields. This reaction proceeds with good functional group tolerance under mild conditions with high efficiency and excellent selectivity. Preliminary biological assays show that some of these compounds display promising activities as CDC25B inhibitor, TC-PTP inhibitor, and PTP1B inhibitor.
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