Acetylation of N-heteroaryl bromides via PdCl(2)/(o-tolyl)(3)P catalyzed Heck reactions

作者：He Tianxiong; Tao Xiaochun^*; Wu Xinyan; Cai Lisheng; Pike Victor W

来源：Synthesis, 2008, (6): 887-890.

DOI：10.1055/s-2008-1032193

• acetylation
• butyl vinyl ether
• isopropanol
• N-heteroaryl bromides

A new user-friendly and convenient method for the acetylation of N-heteroaryl bromides is described. This process is based on the palladium-catalyzed olefination of an N-heteroaryl bromide with butyl vinyl ether, followed by acid hydrolysis of the intermediate heteroaryl vinyl ether in situ. Isopropanol at 85 degrees C, in the presence of K(3)PO(4)center dot 3H(2)O (2 equiv), PdCl(2) (2 mol%) and (o-tolyl)(3)P (4 mol%), provided the best conditions, giving yields of N-heteroaryl bromides up to 75%.

• 出版日期2008-3-18
• 单位华东理工大学