Halogenation of Pyrazolo[1,5-a]Pyrimidines with NXS

被引:3
|
作者
Sang, Tian [1 ]
Li, Chuntian [1 ]
Jia, Fan [1 ]
He, Jing [1 ]
Liu, Yan [1 ]
Vaccaro, Luigi [2 ]
Liu, Jichang [1 ]
Liu, Ping [1 ]
机构
[1] Shihezi Univ, Sch Chem & Chem Engn, Key Lab Green Proc Chem Engn Xinjiang Bingtuan, Shihezi, Peoples R China
[2] Univ Perugia, Dipartimento Chim Biol & Biotecnol, Lab Green SOC, Perugia, Italy
基金
中国国家自然科学基金;
关键词
Halogenation; pyrimidine; synthesis; RECEPTOR; POTENT;
D O I
10.1080/10406638.2022.2144906
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A series of halogenated systems for pyrazolo[1,5-a]pyrimidines have been developed. Selective transformations of pyrazolo[1,5-a]pyrimidines by mono- and di-iodination were achieved by varying the ratio of pyrazolo[1,5-a]pyrimidines to NIS. In addition, the reaction of pyrazolo[1,5-a]pyrimidines with NBS or NCS uniquely gave dibrominated or dichlorinated products. The wide range of substrates, good functional group tolerance and gram-scale synthesis further demonstrate the application potential of this reaction. This work provides an efficient method for the construction of structurally diverse halogenated pyrazolo[1,5-a]pyrimidine derivatives.
引用
收藏
页码:8037 / 8047
页数:11
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