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Benzo[c][2,7]naphthyridines as inhibitors of PDK-1.苯并[c][2,7]萘啶作为丙酮酸脱氢酶激酶-1（PDK-1）的抑制剂
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A novel and efficient one step synthesis of 2-amino-5-cyano-6-hydroxy-4-aryl pyrimidines and their anti-bacterial activity.2-氨基-5-氰基-6-羟基-4-芳基嘧啶的新型高效一步合成及其抗菌活性
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在水中高效合成 2-烷基硫代-4-氨基-5-氰基-6-芳基（烷基）嘧啶的三组分一锅法。

An efficient three-component, one-pot synthesis of 2-alkylthio-4-amino-5-cyano-6-aryl(alkyl)pyrimidines in water.

机构信息

State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191, People's Republic of China.

出版信息

Mol Divers. 2012 Aug;16(3):431-9. doi: 10.1007/s11030-012-9376-z. Epub 2012 Jun 28.

DOI:10.1007/s11030-012-9376-z
PMID:22740103
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7088670/
Abstract

A convenient and practical method for the synthesis of 2-alkylthio-4-amino-5-cyano-6-aryl(alkyl)pyrimidines has been developed via a three-component, one-pot reaction from aldehydes, malononitrile and S-alkylisothiouronium salts in water at room temperature. A series of polysubstituted pyrimidines were prepared by this method in moderate to excellent yields. In addition, two kinds of pyrimidine-fused heterocyclic derivatives with potential pharmacological activity were constructed from our 2-alkylthio-4-amino-5-cyano-6-arylpyrimidines.

摘要

一种方便实用的 2-烷硫基-4-氨基-5-氰基-6-芳基（烷基）嘧啶的合成方法，通过在水相中室温下，由醛、丙二腈和 S-烷基亚硫脲盐进行三组分一锅反应来实现。通过该方法可以中等至优异的收率制备一系列多取代嘧啶。此外，还可以从我们的 2-烷硫基-4-氨基-5-氰基-6-芳基嘧啶构建具有潜在药理活性的两种嘧啶稠合杂环衍生物。