Microwave-assisted synthesis of pyrimidine libraries

被引：86

作者：

Bagley, MC ^{[1
]}

Hughes, DD ^{[1
]}

Lubinu, MC ^{[1
]}

Merritt, EA ^{[1
]}

Taylor, PH ^{[1
]}

Tomkinson, NCO ^{[1
]}

机构：

[1] Cardiff Univ, Sch Chem, Cardiff CF10 3TB, S Glam, Wales

来源：

QSAR & COMBINATORIAL SCIENCE | 2004年 / 23卷 / 10期

基金：

英国工程与自然科学研究理事会;

关键词：

pyrimidines; microwave synthesis; heterocycles; library synthesis;

D O I：

10.1002/qsar.200420044

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Di- or trisubstituted pyrimidine libraries are prepared in good yield by the microwave irradiation of an alkynone and either an amidine or guanidine at 120-150degreesC in acetonitrile in the presence of sodium carbonate or at 100degreesC after treatment with methanolic sodium methoxide in a sealed tube using a monomodal microwave synthesiser. These rapid and efficient methods often require no chromatographic purification and so are appropriate for automated combinatorial methodology and have been applied in the synthesis of a small library of potentially, useful novel ligands for the estrogen receptor based on the pyrimidine template.

引用

页码：859 / 867

页数：9

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