Solution-phase parallel synthesis of S-DABO analogues

被引：12

作者：

Togninelli, A ^{[1
]}

Carmi, C ^{[1
]}

Petricci, E ^{[1
]}

Mugnaini, C ^{[1
]}

Massa, S ^{[1
]}

Corelli, F ^{[1
]}

Botta, M ^{[1
]}

机构：

[1] Univ Siena, Dipartimento Farm Chim Tecnol, I-53100 Siena, Italy

来源：

TETRAHEDRON LETTERS | 2006年 / 47卷 / 01期

关键词：

D O I：

10.1016/j.tetlet.2005.10.142

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A simple and straightforward methodology for the parallel, solution-phase synthesis of a new series of S-DABO derivatives I and 2, bearing aromatic substituents at the C2 and C6 positions, has been developed. Starting from potassium ethyl malonates 3, thiouracil intermediates 5 were prepared through parallel synthesis and isolated as pure products by simple extraction with ethyl acetate. Selective S-benzylation of 5 was achieved in few minutes under microwave irradiation to give the title compounds 1, which were oxidized in parallel to the corresponding sulfones 2. Some of the new compounds 1 showed potent inhibitory activity against HIV-1 RT. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：65 / 67

页数：3

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