基于氰基乙酰胺参与的微波辅助合成吡啶并嘧啶衍生物任务书
2020-07-02 22:58:28
1. 毕业设计(论文)的内容和要求
吡啶并嘧啶类化合物是一类含氮的杂环化合物同时也是构成天然产物的重要组成部分[1],这类化合物一般具有良好的药理活性和生物活性。
比如具有杀菌[2]、抗癌[3]、抗过敏[4]、抗心血管疾病[5]等药理活性。
尽管已经报道过合成此类杂环的许多的方法[6],但多数都具有以下的缺点:反应条件较苛刻,产率较低,反应时间较长;而且使用强酸强碱试剂和金属催化剂,操作步骤较为繁琐。
2. 参考文献
[1]Buron F, Merour J Y, Akssira M, et al. Recent advances in the chemistry and biology of pyridopyrimidines [J]. Eur. J. Med. Chem., 2015, 95: 76-95. [2]Abdel-Rahman A H, Keshk E M, Hanna M A, et al. Synthesis and evaluation of some new spiro indoline-based heterocycles as potentially active antimicrobial agents [J]. Bioorg. Med. Chem., 2004, 12 (9): 2483-2488. [3]Gree D, Vorin S, Manthati V L, et al. The synthesis of new selected analogues of the pro-apoptotic and anticancer molecule HA 14-1 [J]. Tetrahedron Lett., 2008, 49 (20): 3276-3278. [4]Clara C. Blad, Jacobus P. D. van Veldhoven and Corne#769; Klopman, et al. Novel 3,6,7-substituted pyrazolopyrimidines as positive allosteric modulators for the hydroxycarboxylic acid receptor 2 (GPR109A) [J]. J. Med. Chem., 2012, 55: 3563-3567. [5]Lijie Peng, Xuefei Gao and Lei Duan, et al. Identification of pyrido[1,2-α]pyrimidine-4-ones as new molecules improving the transcriptional functions of estrogen-related receptor ɑ [J]. J. Med. Chem., 2011, 54: 7729-7733. [6]Hafiz I S A, Ramiz M M M, Mahmoud F F, et al. β-Enaminonitriles in heterocylic synthesis: Synthesis of new tetrahydropyridinethione, pyridopyrimidines, pyridotriazines and dihydropyridines [J]. Chem. Sci., 2008, 120 (3): 339-345.
3. 毕业设计(论文)进程安排
起讫日期 设计(论文)各阶段工作内容 备 注 2017.12.01~12.22 申报课题并且下达任务书,提出要求,开始查阅文献; 2017.12.23~1.12 查阅文献,并且认真阅读归纳总结完成开题报告; 2018.2.26~3.19 设计实验方案,准备实验材料; 2018.3.20~4.13 化合物的合成; 2018.4.14~5.20 各取代类的化合物合成; 2018. 5.21~6.1 质谱,核磁对结构的确证; 2018. 6.2~ 毕业论文的撰写、修改、成文装订,论文答辩