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毕业论文网 > 任务书 > 化学化工与生命科学类 > 制药工程 > 正文

2-硝基苯酚与芳甲基氯环化制备2-芳基苯并恶唑类化合物研究任务书

 2020-05-04 09:05  

1. 毕业设计(论文)的内容和要求

2-芳基苯并恶唑类化合物作为结构单元在功能材料、活性有机分子、药物分子合成中具有广泛的应用。

常用的制备方法包括2-氨基苯酚在较高温度或氧化剂存在下与醛、酸、苄醇或苄胺缩合反应等。

本课题采用邻硝基苯酚和芳甲基氯为底物,s催化方法进行条件优化进而进行底物适用性研究。

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2. 参考文献

[1] I.J. Turchi and M.J.S. Dewar, Chemistry of oxazoles[J]. Chem. Rev. 1975, 75, 389-437. [2] J. Boyer, E. Arnoult, M. Meuml;debielle, J. Guillemont, J. Unge and D. Jochmans, Difluoromethylbenzoxazole Pyrimidine Thioether Derivatives: A Novel Class of Potent Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors[J]. J. Med. Chem. 2011, 54, 7974-7985. [3] S. Rajasekhar, B. Maiti and K. Chanda, A Decade Update on Benzoxazoles, a Privileged Scaffold in shy;Synthetic Organic Chemistry[J]. Synlett, 2017, 28, 521-541. [4] H. Shama, N. Singh and D.O. Jiang, A ball-milling strategy for the synthesis of benzothiazole, benzimidazole and benzoxazole derivatives under solvent-free conditions[J]. Green Chem. 2014, 16, 4922-4930. [5] M. Bala, P.K. Verma, U. Shama, N. Kumar and B. Singh, Iron phthalocyanine as an efficient and versatile catalyst for N-alkylation of heterocyclic amines with alcohols: one-pot synthesis of 2-substituted benzimidazoles, benzothiazoles and benzoxazoles[J].Green Chem. 2013, 15, 1687-1693. [6] T. Xiao, S. Xiong, Y. Xie, X. Dong and L. Zhou, Copper-catalyzed synthesis of benzazoles via aerobic oxidative condensation of o-amino/mercaptan/hydroxyanilines with benzylamines[J]. RSC Adv. 2013, 3, 15592-15595. [7] B. Maleki, M. Baghayeri, S.M. Vahdat, A. Mohammadzadeh and S. Akhoondi, Ag@TiO2 nanocomposite; synthesis, characterization and its application as a novel and recyclable catalyst for the one-pot synthesis of benzoxazole derivatives in aqueous media[J]. RSC Adv. 2015, 5, 46545-46551. [8] T. Guntreddi, R. Vanjari and K.N. Singh, Elemental Sulfur Mediated Decarboxylative Redox Cyclization Reaction of o-Chloronitroarenes and Arylacetic Acids[J]. Org. Lett. 2015, 17, 976-978. [9] L. Tang, Z. Yang, T. Sun, D. Zhang, X. Ma, W. Rao and Y. Zhou, Unexpected Decarboxylation‐Triggered o‐Hydroxyl‐Controlled Redox Condensation of Phenylglycines with 2‐Nitrophenols in Aqueous Media[J]. Adv. Synth. Catal. 2018, 360, 3055-3062. [10] H. Gan, D. Miao, Q. Pan, R, Hu, X, Li and S. Han, S8‐Mediated Cyclization of 2‐Aminophenols/thiophenols with Arylmethyl Chloride: Approach to Benzoxazoles and Benzothiazoles[J]. Chem. Asian J. 2016, 11, 1770-1774

3. 毕业设计(论文)进程安排

2018.12-2019.1 文献检索,原料等订购,外文翻译,开题报告 2019.2-2019.5 条件筛选、部分底物合成、底物适用性研究及论文撰写 2019.6 答辩

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