Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
5219196 | Tetrahedron | 2012 | 8 Pages |
Abstract
Suzuki-Miyaura cross-coupling reaction with 2-heteroarylboronic acids is generally challenging due to these acids easy decomposition. To overcome this problem, we developed a coupling method that uses 2-heteroaryl pinacol boronates in the presence of 1.0 mol % Pd(OAc)2 and 2.0 mol % S-Phos with 4 equiv amount of LiOH in dioxane and H2O at 80 °C for 30 min. This developed method allowed for the synthesis of a wide variety of 2-heteroaryl pyrimidines from 2-chloropyrimidyl derivatives in high yields, and is also useful in the preparation of various biaryl derivatives from heteroaryl chlorides.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Shigehiro Asano, Seiji Kamioka, Yoshiaki Isobe,