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

作者：Molander Gary A^*; Trice Sarah L J; Tschaen Brittany

来源：Tetrahedron, 2015, 71(35): 5758-5764.

DOI：10.1016/j.tet.2015.04.026

• Bis-boronic acid
• Tetrahydroxydiboron
• Borylation
• Cross-coupling

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.

• 出版日期2015-9-2