Preparation of a 7-arylthieno[3,2-d]pyrimidin-4-amine library

作者：Peng Jinsong; Lin Wenqing; Jiang Dahong; Yuan Shixue; Chen Yuanwei^*

来源：Journal of Combinatorial Chemistry, 2007, 9(3): 431-436.

DOI：10.1021/cc0601534

A focused kinase library of 7-arylthieno[3,2-d]pyrimidin-4-amine analogues is readily prepared via solution-phase parallel synthesis. This strategy relies on a key cyclization of a 3-aminothiophene-2-carboxamide with a formamide to construct the thienopyrimidine core. Further elaborations of this core via substitution and Suzuki coupling reactions allow the introduction of other diversity points. This methodology is demonstrated through the preparation of a 72-membered library of 7-arylthieno[3,2-d]pyrimidin-4-amines in good yields and high purities.

• 单位
  中国科学院; 中国科学院成都有机化学有限公司