An efficient synthesis of 1,3-disubstituted 5-diethoxyphosphoryluracils

被引:5
|
作者
Pieta, Marlena [1 ]
Kedzia, Jacek [1 ]
Janecki, Tomasz [1 ]
机构
[1] Lodz Univ Technol TUL, Inst Organ Chem, PL-90924 Lodz, Poland
关键词
5-Diethoxyphosphoryluracils; Diethoxyphosphorylacetamides; N; N-Dimethylformamide-dimethyl acetal; Phosgene; ANTI-HIV ACTIVITY; DERIVATIVES; 5-FLUOROURACIL; ANTI-HIV-1; DIALKYL; POTENT; ACID;
D O I
10.1016/j.tetlet.2015.02.094
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
An efficient three-step procedure for the synthesis of 1,3-disubstituted 5-diethoxyphosphoryluracils is presented. The starting 2-diethoxyphosphorylacetamides were subjected to dimethylaminomethylidenation using N,N-dimethylformamide-dimethyl acetal and the 3-dimethylamino-2-diethoxyphosphorylpropenamides obtained were transformed into N,N'-disubstituted 3-amino-2-diethoxyphosphorylpropenamides by treatment with various amines. Cyclization in the presence of phosgene led to an efficient formation of the title compounds. (C) 2015 Elsevier Ltd. All rights reserved.
引用
收藏
页码:1891 / 1893
页数:3
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