Organic Pharmaceutical Chemistry, Department of Medicinal Chemistry BMC, Uppsala University, Box 574, SE-751 23, Uppsala, Sweden.
Org Lett. 2012 May 4;14(9):2394-7. doi: 10.1021/ol300813c. Epub 2012 Apr 17.
A fast and convenient synthesis of arylamidines starting from readily available potassium aryltrifluoroborates and cyanamides is reported. The coupling was achieved by Pd(II)-catalysis in a one step 20 min microwave protocol using Pd(O(2)CCF(3)), 6-methyl-2,2'-bipyridyl, TFA, and MeOH, providing the corresponding arylamidines in moderate to excellent yields.
本文报道了一种从易得的芳基三氟硼酸钾和氰酰胺出发快速便捷合成芳基脒的方法。该偶联反应在 Pd(II)催化下,通过一步 20 分钟微波法,使用 Pd(O(2)CCF(3))、6-甲基-2,2'-联吡啶、TFA 和 MeOH 进行,以中等至优秀的收率得到相应的芳基脒。