An improved preparation of arylboronates: Application in one-pot Suzuki biaryl synthesis

被引:109
作者
Zhu, L [1 ]
Duquette, J [1 ]
Zhang, MB [1 ]
机构
[1] Bayer Res Ctr, Dept Chem Res, West Haven, CT 06516 USA
关键词
D O I
10.1021/jo0269114
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
We have developed a modification of the Miyaura arylboronate synthesis(1a) by substituting a ligandless palladium catalyst for PdCl2(dppf). Palladium acetate, free of ligand, was found highly effective for such coupling reactions. This modified procedure is advantageous over the original Miyaura synthesis in ease of workup, catalyst removal, and low catalyst cost: Furthermore, the boronates formed in this manner can be used directly for Suzuki coupling reactions in a one-pot fashion. The biaryl products have improved impurity profiles and reduced heavy metal contamination.
引用
收藏
页码:3729 / 3732
页数:4
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