Preparation of 6-Unsubstituted 3,4-Dihydropyrimidin-2(1H)-Ones and 2-(Arylamino)Pyrimidines

作者：Terentjeva S; Muceniece D; Lusis V^*

来源：Chemistry of Heterocyclic Compounds, 2014, 49(12): 1757-1769.

DOI：10.1007/s10593-014-1428-0

• 2-(arylamino)pyrimidines
• 2-chloropyrimidines
• 2-oxo-1,2-dihydropyrimidines
• 2-oxo-1,2,3,4-tetrahydropyrimidines
• Biginelli reaction

The Biginelli reaction of methyl propiolate and of methyl 3-diethylaminoacrylate has yielded a novel series of 6-unsubstituted 3,4-dihydropyrimidin-2(1H)-ones. The successie oxidation of the pyrimidine ring, chlorination of the 2-oxo group, and substitution of the chlorine atom by an aromatic amine give previously unknown 2-(arylamino)pyrimidines. 2-Oxo- and 2-(arylamino)pyrimidine-5-carboxylic acids have been obtained.

• 出版日期2014-3