ACS combinatorial science

Efficient solution-phase synthesis of 4, 5, 7-trisubstituted pyrrolo [3, 2-d] pyrimidines

W Zhang, J Liu, MA Stashko…

文献索引：Zhang, Weihe; Liu, Jing; Stashko, Michael A.; Wang, Xiaodong ACS Combinatorial Science, 2013 , vol. 15, # 1 p. 10 - 19

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摘要

We have developed an efficient and robust route to synthesize 4, 5, 7-trisubstituted pyrrolo [3, 2-d] pyrimidines as potent kinase inhibitors. This solution-phase synthesis features a SNAr substitution reaction, cross-coupling reaction, one-pot reduction/reductive amination and N-alkylation reaction. These reactions occur rapidly with high yields and have broad substrate scopes. A variety of groups can be selectively introduced into the N5 and C7 ...