Synthesis and Biological Activity of Azaclozodihypyrimidine and Pyrimidine Derivatives

doi:10.6023/cjoc201804020

Chin. J. Org. Chem. ›› 2018, Vol. 38 ›› Issue (12): 3278-3285.DOI: 10.6023/cjoc201804020 Previous Articles Next Articles

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氮杂环并二氢嘧啶及嘧啶衍生物的合成及生物活性评价

张平竹, 王晓芬, 郑雪阳, 连平平, 魏超, 李小六

河北大学化学与环境科学学院河北省化学生物学重点实验室河北大学药物化学与分子诊断教育部重点实验室保定 071002

收稿日期:2018-04-11 修回日期:2018-07-19 发布日期:2018-08-14
通讯作者: 李小六 E-mail:lixl@hbu.cn
基金资助:
国家自然科学基金（Nos.21572044，21372060，21172051）、河北省自然基金（No.B2016201031）、教育部长江学者创新团队发展计划（No.IRT_15R43）、河北省高等学校科学技术研究（No.QN2017015）资助项目.

Synthesis and Biological Activity of Azaclozodihypyrimidine and Pyrimidine Derivatives

Zhang Pingzhu, Wang Xiaofen, Zheng Xueyang, Lian Pingping, Wei Chao, Li Xiaoliu

Key Laboratory of Chemical Biology of Hebei Province, Key Laboratory of Medicinal Chemistry and Molecular Diagnosis of Ministry of Education, School of Chemistry and Environmental Science, Hebei University, Baoding 071002

Received:2018-04-11 Revised:2018-07-19 Published:2018-08-14
Contact: 10.6023/cjoc201804020 E-mail:lixl@hbu.cn
Supported by:
Project supported by the National Natural Science Foundation of China (Nos. 21572044, 21372060, 21172051), Hebei Natural Science Foundation (No. B2016201031) and Program for Changjiang Scholars and Innovative Research Team in University (No. IRT-15R43), the Colleges and Universities Science Technology Research Project of Hebei Province (No. QN2017015).

1. Synthesis and Biological Activity of Azaclozodihypyrimidine and Pyrimidine Derivatives.PDF(965KB)

Abstract

A series of novel aryl-substituted imidazo[1,2-a]pyrimidine and triazolo[1,5-a] pyrimidine were synthesized by the tandem reaction of Knoevenagel and Atwal modified Biginelli, following by aromatization. Some of their cytotoxic activities against Hela and A549 cells and inhibition for apple tree canker were preliminarily evaluated.

Key words: Knoevenagel reaction, Biginelli reaction, imidazo[1,2-a]dihypyrimidine, imidazo[1,2-a]pyrimidine, triazolo[1,5-a]pyrimidine

Cite this article

Zhang Pingzhu, Wang Xiaofen, Zheng Xueyang, Lian Pingping, Wei Chao, Li Xiaoliu. Synthesis and Biological Activity of Azaclozodihypyrimidine and Pyrimidine Derivatives[J]. Chin. J. Org. Chem., 2018, 38(12): 3278-3285.

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氮杂环并二氢嘧啶及嘧啶衍生物的合成及生物活性评价

Synthesis and Biological Activity of Azaclozodihypyrimidine and Pyrimidine Derivatives

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