Preparation of a 7-arylthieno[3,2-d]pyrimidin-4-amine library.
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.
Peng
Jinsong
J
Key Laboratory of Asymmetric Synthesis & Chirotechnology of Sichuan Province and Union Laboratory of Asymmetric Synthesis, Chengdu Institute of Organic Chemistry, Chinese Academy of Sciences, Chengdu 610041, China.
Lin
Wenqing
W
Jiang
Dahong
D
Yuan
Shixue
S
Chen
Yuanwei
Y
D020650:Combinatorial Chemistry Techniques / Q000379:methods*; D015394:Molecular Structure; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000737:chemistry; D013237:Stereoisomerism
D011743:Pyrimidines