Intramolecular cyclization of imidazo[1,2-a]pyridines via a silver mediated/palladium catalyzed C–H activation strategy
Literature Information
Publication Date
2019-04-30
DOI
10.1039/C9QO00389D
Impact Factor
5.281
Authors
Debasmita Saha, Anupreet Kharbanda, Nkeseobong Essien, Lingtian Zhang, Rose Cooper, Debasish Basak, Samantha Kendrick, Brendan Frett, Hong-yu Li
View Original
Abstract
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.
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Organic Chemistry Frontiers
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