1. 毕业设计（论文）的内容和要求

2-苄基苯并恶唑类化合物作为结构单元在活性天然产物、药物分子合成中具有广泛的应用。

最近报道的制备方法包括2-氨基苯酚在较高温度或氧化剂存在下与醛、二卤代酮、苯乙酸或肉桂酸缩合反应等。

本课题拟采用邻氨基苯酚与苯乙炔在s催化下进行条件优化进而进行底物适用性研究。

2. 参考文献

[1] B. Tekiner-Gulbas, O. Temiz-Arpaci, I. Yildiz and N. Altanlar, Synthesis and in vitro antimicrobial activity of new 2-[p-substituted-benzyl]-5-[substituted-carbonylamino]benzoxazoles[J]. Eur. J. Med. Chem. 2007, 42, 1293-1299. [2] D.R. Chancellor, K.E. Davies, et al. Discovery of 2-Arylbenzoxazoles as Upregulators of Utrophin Production for the Treatment of Duchenne Muscular Dystrophy[J]. J. Med. Chem. 2011, 54, 3241-3250 [3] S. Rajasekhar, B. Maiti and K. Chanda, Synlett A Decade Update on Benzoxazoles, a Privileged Scaffold in shy;Synthetic Organic Chemistry[J]. 2017, 28, 521-541 [4] M.S. Mayo, X. Yu, et al. Synthesis of Benzoxazoles from 2-Aminophenols and β-Diketones Using a Combined Catalyst of Broslash;nsted Acid and Copper Iodide[J]. J. Org. Chem. 2014, 79, 6310-6314. [5] M. Pizzetti, E. De Luca, et al. A General Approach to Substituted Benzimidazoles and Benzoxazoles via Heterogeneous Palladium‐Catalyzed Hydrogen‐Transfer with Primary Amines[J]. Adv. Synth. Catal. 2012, 354, 2453-2464 [6] L. Tang, X. Guo, Y. Yang, Z. Zha and Z. Wang, Gold nanoparticles supported on titanium dioxide: an efficient catalyst for highly selective synthesis of benzoxazoles and benzimidazoles[J]. Chem. Commun. 2014, 50, 6145-6148. [7] C. Yu, X. Guo, et al. AgPd Nanoparticles Deposited on WO2.72 Nanorods as an Efficient Catalyst for One-Pot Conversion of Nitrophenol/Nitroacetophenone into Benzoxazole/Quinazoline[J]. J. Am. Chem. Soc. 2017, 139, 5712-5715. [8]Y. Li, M. Wang, et al. Cobalt-Catalyzed Cross-Dehydrogenative Coupling Reactions of (Benz)oxazoles with Ethers[J]. J. Org. Chem. 2016, 81, 11743-11750. [9] T.B. Nguyen and P. Retailleau. Elemental Sulfur-Promoted Oxidative Rearranging Coupling between o#8209;Aminophenols and Ketones: A Synthesis of 2#8209;Alkyl benzoxazoles under Mild Conditions. Org. Lett. 2017, 19, 3887-3890. [10] Z.-L. Li, L.-K. Jin and C. Cai. Efficient synthesis of 2-substituted azoles: radical C#8211;H alkylation of azoles with dicumyl peroxide, methylarenes and cycloalkanes under metal-free condition[J]. Org. Chem. Front., 2017, 4, 2039#8211;2043.

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