Intramolecular cyclization of imidazo[1,2-a]pyridines via a silver mediated/palladium catalyzed C–H activation strategy

文献情報

出版日 2019-04-30

DOI 10.1039/C9QO00389D

インパクトファクター 5.281

著者

Debasmita Saha, Anupreet Kharbanda, Nkeseobong Essien, Lingtian Zhang, Rose Cooper, Debasish Basak, Samantha Kendrick, Brendan Frett, Hong-yu Li

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要旨

A C–H activation reaction was developed using imidazo[1,2-a]pyridine adducts via an AgOAc-mediated, Pd catalyzed intramolecular cyclization. The reaction was optimized and extensively explored using the Ugi/azide MCR as a tool to rapidly broaden substrate scope. Title compounds were screened against a cancer cell panel, and 6af exhibited selective, antiproliferative activity against the MCF-7 (breast cancer) cell line. This C–H activation methodology can be utilized to rapidly reach new chemical-space for drug discovery.

掲載誌

Organic Chemistry Frontiers

CiteScore: 7.8

自己引用率: 8.7%

年間論文数: 724

Organic Chemistry Frontiers publishes high-quality research from across organic chemistry. Emphases are placed on studies that make significant contributions to the field of organic chemistry by reporting either new or significantly improved protocols or methodologies. Topics include, but are not limited to the following: Organic synthesis Development of synthetic methodologies Catalysis Natural products Functional organic materials Supramolecular and macromolecular chemistry Physical and computational organic chemistry

Intramolecular cyclization of imidazo[1,2-a]pyridines via a silver mediated/palladium catalyzed C–H activation strategy

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