氮杂环并二氢嘧啶及嘧啶衍生物的合成及生物活性评价
收稿日期: 2018-04-11
修回日期: 2018-07-19
网络出版日期: 2018-08-14
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
Received date: 2018-04-11
Revised date: 2018-07-19
Online published: 2018-08-14
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).
利用微波促进，以芳香醛、乙酰乙酸乙酯、2-氨基咪唑或3-氨基-1，2，4-三唑为原料，通过Knoevenagel缩合反应和Atwal改进的Biginelli反应串联，简便、高效地合成了系列新型芳基取代咪唑（三唑）并二氢嘧啶衍生物.对所合成化合物进一步芳构化，得到系列氮杂环并嘧啶类化合物，为此类嘧啶化合物的合成提供一条简便的途径.对所合成的部分化合物进行了体外肿瘤细胞（Hela和A549）的细胞毒性及苹果树腐烂病菌的抑制活性测试.
关键词： Knoevenagel缩合反应; Biginelli反应; 咪唑并二氢嘧啶; 三唑并二氢嘧啶; 氮杂环并嘧啶
张平竹 , 王晓芬 , 郑雪阳 , 连平平 , 魏超 , 李小六 . 氮杂环并二氢嘧啶及嘧啶衍生物的合成及生物活性评价[J]. 有机化学, 2018 , 38(12) : 3278 -3285 . DOI: 10.6023/cjoc201804020
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.
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