A Concise and Efficient Approach to 2,6-Disubstituted 4-Fluoropyrimidines from α-CF3 Aryl Ketones

被引:14
作者
Liu, Fangran [1 ,2 ]
Zhang, Xiaofei [2 ]
Qian, Qun [1 ]
Yang, Chunhao [2 ]
机构
[1] Shanghai Univ, Dept Chem, 99 Shang Da Rd, Shanghai 200444, Peoples R China
[2] Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 555 Zu Chong Zhi Rd, Shanghai 201203, Peoples R China
来源
SYNTHESIS-STUTTGART | 2020年 / 52卷 / 02期
基金
中国国家自然科学基金;
关键词
fluoropyrimidine; alpha-CF3 aryl ketone; metal-free; mild conditions; PYRIMIDINE; INHIBITORS; FLUORINE; DESIGN; CHEMISTRY; DISCOVERY;
D O I
10.1055/s-0039-1690248
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Herein, a concise and efficient protocol to synthesize a series of 2,6-disubstituted 4-fluoropyrimidines as universal and useful building blocks in medicinal chemistry is reported. From readily accessible alpha-CF3 aryl ketones and different amidine hydrochlorides, this method provides a very practical approach to this kind of compounds under mild conditions with good to excellent yields.
引用
收藏
页码:273 / 280
页数:8
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