An Efficient Route to Novel Uracil-Based Drug-Like Molecules

被引:10
作者
Babkov, Denis A. [1 ]
Chizhov, Alexander O. [2 ]
Khandazhinskaya, Anastasia L. [3 ]
Corona, Angela [4 ]
Esposito, Francesca [4 ]
Tramontano, Enzo [4 ]
Seley-Radtke, Katherine L. [5 ]
Novikov, Mikhail S. [1 ]
机构
[1] Volgograd State Med Univ, Dept Pharmaceut & Toxicol Chem, Volgograd 400131, Russia
[2] RAS, Zelinsky Inst Organ Chem, Moscow 119991, Russia
[3] Russian Acad Sci, Engelhardt Inst Mol Biol, Moscow 119991, Russia
[4] Univ Cagliari, Dept Life & Environm Sci, I-09042 Cagliari, Italy
[5] Univ Maryland Baltimore Cty, Dept Chem & Biochem, Baltimore, MD 21250 USA
来源
SYNTHESIS-STUTTGART | 2015年 / 47卷 / 10期
基金
俄罗斯基础研究基金会;
关键词
uracil; benzophenone; Weinreb amide; Grignard coupling; bromination; HIV-1; REVERSE-TRANSCRIPTASE; ACID-DERIVATIVES; INHIBITORS; AGENTS; DESIGN; ANTI-HIV-1; REAGENTS; UPDATE;
D O I
10.1055/s-0034-1380405
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
In order to identify new antiretroviral agents, a series of novel uracil derivatives have been synthesized. Optimized conditions for coupling of Weinreb amides with aromatic Grignard reagents allow the convenient preparation of key benzophenone intermediates in high yields and purities. The use of a modified silyl Hilbert-Johnson reaction affords the target compounds under mild conditions.
引用
收藏
页码:1413 / 1422
页数:10
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