Tetrahedron

Suzuki–Miyaura cross-coupling reaction of aryl and heteroaryl pinacol boronates for the synthesis of 2-substituted pyrimidines

S Asano, S Kamioka, Y Isobe

Index: Asano, Shigehiro; Kamioka, Seiji; Isobe, Yoshiaki Tetrahedron, 2012 , vol. 68, # 1 p. 272 - 279

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Citation Number: 14

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 4equiv amount of LiOH in dioxane and H2O at 80° C for 30min. This developed method allowed for the synthesis of a wide variety of 2- ...