Enantioselective Michael addition using 4(3H)-pyrimidinone

被引：0

作者：

Chen, Yong-Sin ^{[1
]}

Huang, Ming-Hsuan ^{[1
]}

Cheng, Yan-Peng ^{[1
]}

Hou, Duen-Ren ^{[1
]}

机构：

[1] Natl Cent Univ, Dept Chem, 300 Jhong Da Rd, Taoyuan 32001, Taiwan

来源：

JOURNAL OF THE CHINESE CHEMICAL SOCIETY | 2022年 / 69卷 / 08期

关键词：

4-pyrimidinone; enantioselective; Michael addition; organocatalysis; ONE-POT SYNTHESIS; PYRIMIDINONE DERIVATIVES; CONFORMATIONAL-ANALYSIS; FEBRIFUGINE; INHIBITORS; DISCOVERY; ANALOGS; ACID;

D O I：

10.1002/jccs.202200105

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

The framework of 4-pyrimidinones is prevalent in biologically and medicinally important molecules. Here we report that chiral N-substituted 4-pyrimidinones were prepared by an enantioselective, organocatalytic aza-Michael addition of 4(3H)-pyrimidinone (4-hydroxypyrimidine) to alpha,beta-unsaturated 1,4-dicarbonyl compounds for the first time. The reactions were optimized by the choice of solvents, screening Cinchona alkaloid-based bifunctional catalysts, and Michael acceptors to achieve good yields and enantioselectivities.

引用

页码：1462 / 1474

页数：13

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