Thiophenes are crucial chemical building blocks in the fields of medicinal and material chemistry. As such, the CÀ H functionalization of these units is of key importance for developing novel applications. Herein, we report the CÀ H borylation of thiophenes using metal-free transfer CÀ H borylation. When performed on C2-substituted thiophenes, the reaction is selective for the borylation on C5, while C3-substituted thiophenes are borylated on C2, a complementary selectivity from reported CÀ H borylation approaches that typically prefer to borylate at the C5 position. An optimization of the catalytic system was performed. The reaction was shown to work with electronically diverse thiophenes and was also compatible with sensitive functional groups. Computational investigation of the reaction mechanism suggests a Lewis pair CÀ H activation mechanism with a selectivity that is kinetically driven. The methodology developed herein is an economical pathway for the preparation of C2-borylated C3-substituted thiophenes.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.
customersupport@researchsolutions.com
10624 S. Eastern Ave., Ste. A-614
Henderson, NV 89052, USA
This site is protected by reCAPTCHA and the Google Privacy Policy and Terms of Service apply.
Copyright © 2024 scite LLC. All rights reserved.
Made with 💙 for researchers
Part of the Research Solutions Family.