1. 1. 毕业设计（论文）的内容、要求、设计方案、规划等
1.前言
1.1 氰基吡啶的研究
吡啶类化合物最初从煤焦油中提取而来[1]。随着我国经济的增长，对吡啶类化合物市场需求量的增加以及现代合成技术的发展，我国吡啶类化合物的生产、消费和出口已占世界吡啶类化合物的30%[2,3]。许多天然产物或合成的化合物中都含有吡啶结构，它们展示了广谱的生物活性[1~4]。如抗菌[5~7]、降血压[8]、治疗心血管疾病[9]、消炎、止痛以及退烧等药物性能[10,11]，而且还被广泛用于IKK-β的抑制活性研究[12,13]。而且该类化合物同样表现出多种优良的农药活性，如杀虫剂、除草剂、杀菌剂等[14,15]。吡啶类农药作为全球第四代新型农药，不仅高效、低毒、持效期长的特点，而且对人及生物有良好的环境相容性，符合现代农药的发展要求和趋势[16]，使其逐渐成为农药创制的主要方向之一。因此，吡啶化合物的应用非常广泛，深加工前景也相当广阔，是我国亟待发展精细化学品之一。
2. 参考文献（不低于12篇）
[1] [1] C. Temple, Jr. G. A. Rener, W. R. Raud et al.Antimitotic Agents: Structure-activity Studies with some Pyridine Derivatives. J.Med. Chem., 1992, 35: 3686~3690. [2] [2] Y. Zhang, O. A. Pavlova, S. I. Chefer et al. 5-SubstitutedDerivatives of 6-Halogeno-3- ((2-(S)-azetidinyl)methoxy)pyridine and 6-Halogeno-3-((2-(S)-pyrrolidinyl)methoxy)pyridinewith Low Picomolar Affinity for Alpha4beta2 Nicotinic Acetylcholine Receptorand Wide Range of Lipophilicity: Potential Probes for Imaging with Positron EmissionTomography. J. Med. Chem., 2004, 47: 2453~2465. [3] [3] C. -S. Chang, Y. -T. Lin, S. -R. Shih et al.Design, Synthesis, and Antipicornavirus Activity of 1-[5-(4-Arylphenoxy)alkyl]-3-pyridin-4-ylimidazolidin-2-oneDerivatives. J. Med. Chem., 2005, 48: 3522~3535. [4][4] J. F. Zhou, G.X. Gong, F. X. Zhu et al. Microwave Promoted One-potSynthesis of 3-(2-Amino-3-cyano-4-arylpyrid-6-yl) Coumarins. Chin. Chem. Lett., 2009, 20:37~39. [5][5] A. Altundas, S. Ayvaz, E. Logoglu. Synthesisand Evaluation of a Series of Aminocyanopyridines as Antimicrobial Agents. Med.Chem. Res., 2009, 20(1): 1~8. [6] [6] A. R. Gholap, K. S. Toti,F. Shirazi et al. Synthesis and Evaluation of Antifungal Propertiesof a Series of the Novel 2-Amino-5-oxo-4-phenyl-5,6,7,8-tetrahydroquinoline-3-carbonitrileand Its Analogues. Bioorg. Med. Chem., 2007, 15: 6705~6715. [7] [7] K. Gobis, H. Foks, A. Kdzia et al. Synthesis and AntibacterialActivity of Novel Pyridine and Pyrazine Derivatives Obtained from Amidoximes. J.Heterocyclic Chem., 2009, 46: 1271~1279. [8] [8] J. J. Baldwin,E. L. Engelhardt, R. Hirschmann et al. HeterocyclicAnalogues of the Antihypertensive Beta-adrenergic Blocking Agent(S)-2-[3-(ter-butylamino)-2-hydroxypropoxy]-3-cyanopyridine. J. Med. Chem.,1980, 23: 65~70. [9] [9] A. A. Krauze, R. O. Vitolinya, G. V. Zarin'shet al. Synthesis and Cardiovascular Activity of Substituted 3-Cyano-3,4-dihydropyridine-2-thionesand 3-Cyanopyridine-2-thiones. Pharm. Chem. J., 1985, 19: 313~318. [10[10] F. Manna, F. Chimenti, A. Bolasco et al. Anti-inflammatory,Analgesic and Antipyretic 4,6-Disubstituted 3-Cyanopyridine-2-ones and 3-Cyano-2-aminopyridines.Eur. J. Med. Chem., 1992, 27: 627~632. [11[11] F. Manna, F. Chimenti, A. Bolasco et al.Anti-inflammatory, Analgesic and Antipyretic 4,6-Disubstituted 3-Cyano-2-aminopyridines.Eur. J. Med. Chem., 1999, 34: 245~254. [12[12] T. Murata,M. Shimada, S. Sakakibara et al. Synthesis and Structureactivity Relationshipsof Novel IKK-β Inhibitors. Part 3: Orally Active Anti-inflammatory Agents. Bioorg.Med. Chem. Lett., 2004, 14: 4019~4022. [13[13] R. Mahesh, R. V. Perumal, P. V. Pandi.Microwave Assisted Synthesis of 2-(4-Substitutedpiperazin-1-yl)-1,8-naphthyridine-3-carbonitrile as a New Class of Serotonin5-HT3 Receptor Antagonists. Bioorg. Med. Chem. Lett., 2004, 14: 5179~5181. [14[14] 慕长炜，覃兆海．吡啶类农药的研究进展（续）．现代农药，2003,2(3): 4~10. [15[15] G. F. Yang, L.Xu, A. Lu. Synthesis and Bioactivity of Novel Triazolo[1,5-a]pyrimidineDerivatives [3]. Heteroatom Chem., 2001, 12(6): 491~496. [16[16] 韩永奇，韩晨曦．吡啶及吡啶农药前景看好．农化市场十日讯，2010, (10):16~16. [17[16] 丁彩峰，刘芳．氰基吡啶的合成与应用．2007年全国乙醛、醋酸及其衍生物技术、市场研讨会交流论文，2007,(4): 76~81. [18[17] 彭晓宏，沈家瑞．聚（丙烯酸钠4乙烯基吡啶）的生物降解性和功能性研究．高等学校化学学报，1999,20(9): 1466~1469. [19[18] F. Shi, S. J. Tu,F. Fang et al. One-pot Synthesis of 2-Amino-3-cyanopyridine Derivativesunder Microwave Irradiation without Solvent. ARKIVOC, 2005, (i): 137~142. [20[19] T. Kobayashi, S. Sasaki, N. Tomita et al.Synthesis and Structure-activity Relationships of 2-Acylamino-4,6-diphenylpyridineDerivatives as Novel Antagonists of GPR54. Bioorg. Med. Chem., 2010, 18: 3841~3859. [21[20] 刘振香，陈鋆．2-氯-3-氰基吡啶的合成与应用．广东化工，2007,34(5): 56~58. [22[21] S. Borovic, G.Tirzitis, D. Tirzite et al. Bioactive 1,4-Dihydroisonicotinic AcidDerivatives Prevent Oxidative Damage of Liver Cells. Eur. J. Pharmacol., 2006, 537: 12~19. [23[22] N. M. Evdokimov, I. V. Magedov, A. S. Kireev etal. One-step, Three-component Synthesis of Pyridines and 1, 4-Dihydropyridineswith Manifold Medicinal Utility. Org. Lett., 2006, 8: 899~902. [24[23] K. Guo, M. J. Thompson, T. R. K. Reddy et al. MechanisticStudies Leading to a New Procedure for Rapid, Microwave Assisted Generation of Pyridine-3,5-dicarbonitrileLibraries. Tetrahedron, 2007, 63: 5300~5311. [25[24] 朱水莲．试验室化学药品、试剂、标准物质管理．冶金分析，2004，(26)：784-786． [26[25] 杨妙贤．农业院校实验室化学药品的安全管．农业与技术，2004，24(5)：175177． [27[26] 韦小杰，张冬云，陈小鹏，等．化工专业实验室管理信息系统的开发与应用．中国现代教育装备，2008，3：2022． [28[27] 冷士良．精细化工实验技术．北京：化学工业出版社，2005：l15． [29[28] 蒋军成，虞汉华．危险化学品安全技术与管理．北京：化学工业出版社，2005：102． [30[29] 莫巍．浅谈实验室化学药品的规范化绿色化管．农业综述，2007，6:5.
|
