一种利用双硼酸进行钯催化芳基和杂芳基卤化物的硼化/铃木-宫浦交叉偶联的改进方法。
A modified procedure for the palladium catalyzed borylation/Suzuki-Miyaura cross-coupling of aryl and heteroaryl halides utilizing bis-boronic acid.
作者信息
Molander Gary A, Trice Sarah L J, Tschaen Brittany
机构信息
Roy and Diana Vagelos Laboratories, Department of Chemistry, University of Pennsylvania, Philadelphia, Pennsylvania 19104-6323.
出版信息
Tetrahedron. 2015 Sep 2;71(35):5758-5764. doi: 10.1016/j.tet.2015.04.026.
Abstract
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.
摘要
报道了一种改进的钯催化形成芳基和杂芳基硼物种的方法，以及使用原子经济性的四羟基二硼（双硼酸，BBA）进行两步一锅法硼化/铃木-宫浦交叉偶联反应。通过使用乙二醇作为添加剂，新方法提高了产率，降低了BBA用量，缩短了反应时间，并扩大了反应范围，包括以前有问题的底物如杂环化合物。
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