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

来源：

POLYCYCLIC AROMATIC COMPOUNDS | 2023年 / 43卷 / 09期

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

页码：8037 / 8047

页数：11

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