A modified procedure for the palladium catalyzed borylation/Suzuki-Miyaura cross-coupling of aryl and heteroaryl halides utilizing bis-boronic acid

TETRAHEDRON

卷:71

Article

Molander, Gary A.¹  Trice, Sarah L. J.¹  Tschaen, Brittany¹ 

[1] Univ Penn, Dept Chem, Roy & Diana Vagelos Labs, Philadelphia, PA 19104 USA

关键词: Bis-boronic acid;    Tetrahydroxydiboron;    Borylation;    Cross-coupling;   

DOI  :  10.1016/j.tet.2015.04.026

来源: Elsevier

【 摘 要 】

A modified Pd-catalyzed method of forming aryl- and heteroarylboron species and a two-step, one-pot borylation/Suzuki-Miyaura cross coupling using the atom economical tetrahydroxydiboron (bis-boronic acid, BBA) is reported. By using ethylene glycol as an additive, the new method results in increased yields, lower BBA loading, faster reaction times, and a broader reaction scope, including previously problematic substrates such as heterocycles. (C) 2015 Elsevier Ltd. All rights reserved.

【 授权许可】

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