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Updated: Jun 4, 2025

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
C(sp3)-H Bond Functionalization of 8-Methylquinolines
Diksha Parmar1, Rohit Kumar1,2, Upendra Sharma1
1C-H Activation & Phytochemistry Lab, Chemical Technology Division, CSIR-IHBT, Palampur, HP 176061, India.
Abstract:
Quinolines have emerged as essential components in various medicinal agents, playing a key role in treating various ailments. Numerous drugs with a quinoline core have been recognized for their antimalarial, antibacterial, and anticancer activities and have been successfully commercialized, including chloroquine, ciprofloxacin, topotecan, etc. Over the past two decades, a tremendous expansion in the C-H bond functionalization of quinoline scaffolds to widen this chemical space for drug discovery have been witnessed. This review article summarizes the efforts toward C(sp3)-H functionalization of 8-methylquinolines for C(sp3)-C/X bond formation under metal and metal-free strategies. Each section briefly overviews the C(sp3)-H functionalization of 8-methylquinoline, highlighting the metal and metal-free approaches.
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