Palladium(ii) catalyzed site-selective C–H olefination of imidazo[1,2-a]pyridines?
Organic & Biomolecular Chemistry Pub Date: 2021-10-20 DOI: 10.1039/D1OB01683K
Abstract
Herein, we disclose an efficient Pd(II)-catalyzed site selective C8 alkenylation of imidazo[1,2-a]pyridines with electronically biased olefinic substrates. Notably, besides the presence of four C–H sites available, selective mono-alkenylation was achieved by N-chelation overriding O-chelation. The versatility and scalability of the catalysis enabled the selective late-stage functionalization of a marketed drug, zolimidine. Various substituted heteroaryl alkenes can be afforded with moderate to good yields with high C8 regioselectivity.
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Journal Name:Organic & Biomolecular Chemistry
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CAS no.: 89640-58-4