Palladium-Catalyzed Highly Regioselective C6 Arylation of Pyrrolo[2,3-d]pyrimidine Derivatives with Arylboronic Acids

被引:9
|
作者
Liu, Min [1 ]
Shen, Chunwei [1 ]
Tang, Ting [2 ]
Pan, Chenhong [1 ]
Liu, Mingrui [1 ]
Zhang, Xingxian [1 ]
机构
[1] Zhejiang Univ Technol, Coll Pharmaceut Sci, Hangzhou 310014, Peoples R China
[2] Hangzhou Normal Univ, Sch Publ Hlth, Hangzhou 311121, Peoples R China
基金
中国国家自然科学基金;
关键词
H ARYLATION; HETEROARENES; BONDS; (HETERO)ARENES; ALKENYLATION; ACTIVATION; INHIBITOR; SP(2); MILD;
D O I
10.1021/acs.orglett.3c00680
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A mild and selective C6 arylation strategy for pyrrolo[2,3-d]pyrimidine derivatives with arylboronic acids at room temperature is described. This unified protocol has been achieved by the synergistic combination of Pd(II)/TEMPO catalysis and CF3CO2H promotion under silver-, base-, and additive-free conditions. The broad substrate scope, good functional group tolerance, excellent regioselectivity, and air and moisture tolerant conditions make this process attractive for the effective synthesis and modification of targeted small molecule drugs.
引用
收藏
页码:2637 / 2641
页数:5
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