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Updated: Jan 7, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives

Facile Preparation of 4-Substituted Quinazoline Derivatives

Published on: February 15, 2016

キノリンスルホンアミドの、ベンチで安定なSO2代替物を用いたアミノスルホニル化による直接的な合成法

Lipat Kaur¹, Rahul Jain¹

¹Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research, S. A. S. Nagar, Punjab 160062, India.

The Journal of organic chemistry

|December 25, 2025

Abstract:

In this study, we utilize inexpensive, bench-stable, and nontoxic K₂S₂O₅ as a surrogate for SO₂ in a palladium-catalyzed one-pot, two-step synthesis of quinoline sulfonamides. The protocol exhibits broad substrate tolerance, accommodating a wide range of amines and substituted quinolines, affording sulfonamides in 25-92%. We obtained mechanistic insights through time-dependent reaction monitoring and control experiments. The methodology was successfully extended to synthesizing an antiproliferative analogue and the one-pot diaminosulfonylation of 3,6-diiodoquinoline, demonstrating its versatility and scalability.

キーワード:

キノリンスルホンアミドアミノスルホニル化二酸化硫黄代替物パラジウム触媒有機合成

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