生物活性分子的合成及应用、连续流微反应工艺、创新药物研发、有机荧光材料

一、近年主持的科研项目

1.       创新小分子农药研发四川省自然科学基金创新研究群体（2023NSFSC1977），四川省科技厅项目，2023.01，负责人

2.       溶剂调控多色发光碳化聚合物点的分子态发光机制及应用研究（2022ZYD0048），省科技厅项目，2022.09，负责人

3.       硝基二甲苯的连续流生产工艺研究，企、事业单位委托，2022.07，负责人

4.       抗病毒新药巴洛沙韦酯合成工艺关键技术研究（2021YFG0291），省科技厅项目，2021.04，第二单位负责人

5.       硝基二甲苯的连续流生产工艺及产能提升研究（2021YG02），宜宾市科技局项目，2021.01，负责人

6.       基于植物活性物质研究，企业委托，2021.03，负责人

7.       新型生物除草剂的创制，企业委托，2020.03，负责人

8.       微通道间二甲苯硝化安全工艺研发（2019GY007），宜宾市科技局项目，负责人

9.       地奥司明微反应制备工艺研究，省科技厅项目，2019.01，第二单位负责人

10.    杀螨型植物精油活性成分的研究，企业委托，2019.08，负责人

11.    基于先导化合物结构优化的新药研究与开发（18TD0023），四川省教育厅项目，2017.10，负责人

12.    系列农用杀虫剂杀菌剂的研发，企业委托，2018.04，负责人

13.    未知化合物结构鉴定、合成、生产评估，企业委托，2018.04，负责人

14.    以天然植物源农药有效成份为先导化合物的新型高效、低毒农药杀菌剂的创制（2017NZ0048），省科技厅项目，2017.03，第二单位负责人

15.    手性抗肺癌药物Crizotinib的创新工艺研究（2015-HM01-00366-SF），成都市科技局，     2017.06，负责人

16.    植物源农药先导化合物的结构改性及优化，企业委托，2017.01，负责人

17.    手性胺类全新IDO抑制剂的设计、合成及活性研究（2017JQ0023），省科技厅项目，2017.03，负责人

18.    碳碳双键还原小试工艺研究，企业委托，2017.02，负责人

19.    系列农用杀菌剂的制备，企业委托，2016.02，负责人

20.    先导化合物XZY-3、XZY-5和XZY-9 的结构改性及优化，企业委托，2016.03，负责人

21.    抗肿瘤新药克里唑替尼的创新工艺研究（14CZ0014），四川省教育厅项目，2014.01，负责人

22.    手性抗衡阴离子导向的不对称催化Ritter-type反应（21102115），国家自然科学基金项目，2012.01，负责人

二、科研成果、专利及奖励（部分）

1. 一种绿色的选择性还原共轭双键的方法，专利号：ZL201310421707.5，第一发明人

2. 一种N-（β-硝基烷基）酰胺类化合物的制备方法，专利号：ZL201410097899.3，第一发明人

3. 一种酰胺类化合物的制备方法，专利号：ZL201410736723.8，第一发明人

4. 一种硝基芳香醇的制备方法，专利号：ZL201410737566.2，第一发明人

5. 一种选择性还原4-硝基苯乙腈和醛缩合反应产物的方法，专利号：ZL 201510563570.6，第一发明人

6. 三乙烯二胺在催化芳香醛与硝基烃反应生成硝基芳香醇中的催化剂用途，专利号：ZL 201410738325.X，第一发明人

7. 手性α-苯乙醇的优先结晶制备方法，专利号：ZL201510797259.8，第一发明人

8. 一种克里唑替尼的制备方法，专利号：ZL201510725648.X，第一发明人

9. 取代氰基乙酸酯化合物的无溶剂制备方法，专利号：ZL201610183661.1，第一发明人

10. 吡啶骈[3,4-b]吲哚脲类化合物及其作为IDO抑制剂的用途，专利号：ZL201610103753.4，第一发明人

11. 一种制备α-烷基-β-酮酯类化合物的方法，专利号：ZL201610814221.1，第一发明人

12. 1H-吲唑类衍生物及其作为IDO抑制剂的用途，PCT/CN2016/099845，第一发明人

13. 一种没食子酸衍生的农用杀菌剂及用途，专利号：ZL201710811095.9，第一发明人

14. 双取代对硝基苯乙腈衍生物的无溶剂制备方法，专利号：ZL201710994932.6，第一发明人

15. 一种手性吡啶磺酰酯类化合物的制备及应用, 专利号：ZL2018100986964，第一发明人

16. 具有吲哚胺-2,3-双加氧酶（IDO）抑制剂活性的咪唑甲胺类衍生物及其合成方法，专利号：ZL2018102417262，第一发明人

三、近五年发表的科研论文 （部分）

[1]            Chengshuang Liao, Feishi Shan, Yinxia Zhu, Haodong Mi, Yanhong Liu, Qiao Song, Chuanfeng Wang, Leyong Wang * , Zhouyu Wang*. Self-ratiometric Photoluminescence Carbonized Polymer Dots with Junas Structure for Hypochlorite Selective Sensing. Sensor. Actuat. B-Chem., 2024, 420, 136453.

[2]            Li Yan, Chengshuang Liao, Yinxia Zhu, Haodong Mi, Shanshan Jiang, Feishi Shan, Yanhong Liu, Yahui Zhang, Qian Zhou,  Zhouyu Wang*, Xiaoqi Yu, Carbonized Polymer Dots with Aggregation-Induced Effect for Type I Photodynamic Therapy，ACS Applied Nano Materials, 2023, 6 (14):13320-13329.

[3]            Yahui Zhang, Haoyu Xia, Mengdie Yang, Hairong Li, Feishi Shan, Yilong Chen, Xue Yue, Zhouyu Wang*, Xiaoqi Yu*, Carbon dots with two-photon fluorescence imaging for efficient synergistic trimodal therapy, Chinese Chemical Letters,2023, 34 (09): 108197.

[4]            Feishi Shan, Tingrui Zhang, Chengshuang Liao, Jing Zhang, Li Yan, Yanman Liu, Zhixing Cao, Min Wang, Yahui Zhang, Leyong Wang, Zhouyu Wang*, Xiaoqi Yu, Red/NIR emission carbonized polymer dots based on citric acid-benzoylurea and their application in lymph nodes imaging，Chinese Chemical Letters. 2023, 34(11):108402.

[5]            Feishi Shan, Jing Zhang, Chengshuang Liao, Zhouyu Wang*, Leyong Wang*，Mechanisms of photoluminescence in the molecular state of carbon dots prepared from o-phenylenediamine，Chinese Chemical Letters. 2023, 34(07): 108107.

[6]            Qian Zhou, Shanqiang Wang, Xiaoyun Ran, Linzhi Shen, Xiaolin Luo, Gui Wang ,Hui Yang, Zhouyu Wang*, Xiaoqi Yu*, The water-soluble bicyclic 2-pyridone-based fluorescent probe for fast and selective detection of hypochlorite. Chinese Chemical Letters. 2023, 34(11):107922.

[7]            Yahui Zhang, Hairong Li, Mengdie Yang, Wenbo Dai, Jianbing Shi, Bin Tong,  Zhengxu Cai*, Zhouyu Wang*, Yuping Dong, Xiaoqi Yu*, Organic room-temperature phosphorescencematerials for bioimaging, Chem. Commun., 2023, 59, 5329–5342.

[8]             Xiao-Long He, You-Wu Wen, Hechen Li, Shan Qian,* Mengyang He, Qiao Song, and Zhouyu Wang*，Diastereoselective Synthesis of Dihydrobenzofuran-Fused Spiroindolizidines via Double-Dearomative [3 + 2] Cycloadditions，J. Org. Chem. 2023, 88, 493−503.

[9]            Qiao Song *, Sheng Wang, Xiangui Lei, Yan Liu , Xin Wen and Zhouyu Wang,* One-Pot Route from Halogenated Amides to Piperidines and pyrrolidines，Molecules，2022，27，4698-4705.

[10]         Qiao Song*, Xiangui Lei , Sheng Yang , Sheng Wang , Jianhui Wang , Jiujun Chen , Yong Xiang, Qingwu Huang and Zhouyu Wang*，Continuous-flow Synthesis of Nitro-o-xylenes: Process Optimization, Impurity Study and Extension to Analogues，Molecules， 2022， 27， 5139-5148.

[11]         Feishi Shan, Lijuan Fu, Xiangyu Chen, Xiangyan Xie, Chengshuang Liao, Yinxia Zhu,Haoyu Xia, Jing Zhang, Li Yan, Zhouyu Wang*, Xiaoqi Yu*, Waste-to-wealth: functional biomass carbon dots based on bee pollen waste and application，Chin. Chem. Lett.，2022, 33, 2942-2948.

[12]         Yuxiang Wu, Dan Ren, Cheng Gao, Junyan Li, Bo Du, Zhouyu Wang*, Shan Qian*, Recent advances for alkaloids as botanical pesticides for use in organic agriculture, International Journal of Pest Management, 2021, https://doi.org/10.1080/09670874.2021.1917723.

[13]         Xiao-Long He, Cheng Wang, You-Wu Wen, Yi-Bing Zhao, Huan Yang, Shan Qian, Lingling Yang* and Zhouyu Wang*, Highly stereoselective dearomatizative [3+2] cycloadditon of cyclic pyridinium ylides to access spiro-indolizidine scaffolds. Org. Chem. Front., 2021, 8,    5847-5851.

[14]         Xiao-Long He, Cheng Wang, You-Wu Wen, Zhouyu Wang,* and Shan Qian*, Recent Advances in Catalytic Atroposelective Construction of Pentatomic Heterobiaryl Scaffolds. ChemCatChem. 2021, 13, 3547 – 3564.

[15]         Xiaoyun Ran, Qian Zhou, Jin Zhang, Shanqiang Wang, Gui Wang, Hui Yang,   Xiaochun Liu,  Zhouyu Wang* and  Xiaoqi Yu*, A solvent-free and efficient synthesis of bicyclic 2-pyridone derivatives for endoplasmic reticulum imaging, Organic Chemistry Frontiers, 2021, 8, 3631-3638.

[16]         Qiao Song, Yan Liu, Linlin Cai, Xinyu Cao, Shan Qian *, Zhouyu Wang *, One-pot tandem route to fused indolizidines and quinolizidines: Application in the synthesis of alkaloids and bioactive compounds. Chinese Chemical Letters, 2021, 32, 1713–1716.

[17]         Feishi Shan, Haoyu Xia, Xiangyan Xie, Lijuan Fu, Hui Yang, Qian Zhou, Yuanyuan Zhang, Zhouyu Wang*, Xiao Qi Yu. Novel N-doped carbon dots prepared via citric acid and benzoylurea by green synthesis for high selectivity Fe(III) sensing and imaging in living cells.Microchemical Journal, 2021,167, 106273-106283.

[18]         Xiaoyun Ran, Yan Long, Sheng Yang, Changjiang Peng, Yuanyuan Zhang, Shan Qian, Zhenju Jiang, Xiaomei Zhang,  Lingling Yang, Zhouyu Wang* and Xiaoqi Yu*，A novel route to unsymmetrical disubstituted ureas and thioureas by HMPA catalyzed reductive alkylation with trichlorosilane，Org. Chem. Front., 2020, 7, 472-481.

[19]         Huan Yang, Wanying Zhang, Sumudu Athukorale, Zhiguo Liu, Shengli Zou, Bruno Donnadieu, Zhouyu Wang*, and Dongmao Zhang*，Dithiosulfindene Adsorption and Reaction on Gold Nanoparticles in Water，J. Phys. Chem. C2020, 124, 686−692.

[20]         Hui Liu, Yingkun Yan, Jiayan Zhang, Min Liu, Shaobing Cheng, Zhouyu Wang* and Xiaomei Zhang*, Enantioselective dearomative [3+2] annulation of 5-amino-isoxazoles with quinone monoimines, Chem. Commun., 2020, 56, 13591-13594.

[21]         Jiayan Zhang, Min Liu, Min Huang, Hui Liu, Yingkun Yan, Zhouyu Wang* and Xiaomei Zhang*, Enantioselective dearomative [3 + 2] annulation of 3-hydroxy chromanones with azonaphthalenes, Org. Chem. Front., 2020, 7, 3160–3165.

[22]         Wei Xu, Hao Yao, Xing Zhang, Changjiang Peng, Ling Li, Yuanyuan Zhang, Shan Qian, Lingling Yang,* Zhouyu Wang*, K2CO3 Promoted Cascade Reaction for the Preparation of 1H-Imidazol-4-yl-1-amine Derivatives, Letters in Organic Chemistry, 2020, 17, 127-132.

[23]         Lingling Yang, Feng Chen, Cheng Gao, Jiabao Chen, Junyan Li, Siyan Liu, Yuanyuan Zhang, Zhouyu Wang*, Shan Qian*. Design and synthesis of tricyclic terpenoid derivatives as novel PTP1B inhibitors with improved pharmacological property and in vivo antihyperglycaemic efficacy, Journal of  Enzyme Inhibition and Medicinal Chemistry, 2020, 35, 152-164.

[24]         Lijiao Wang, Chao Li , Wei Chen , Chen Song , Xing Zhang , Fan Yang , Chen Wang , Yuanyuan Zhang , Shan Qian , Zhouyu Wang* and Lingling Yang*, Discovery of (5-Phenylfuran-2-yl)methanamine Derivatives as New Human Sirtuin 2 Inhibitors, Molecules, 2019, 24, 2724.

[25]         Huan Yang, Guanglin Weng, Dongmei Fang, Changjiang Peng, Yuanyuan Zhang, Xiaomei Zhang* and Zhouyu Wang*，Enantioselective Conjugate Hydrosilylation of α,β-Unsaturated Ketones，RSC Adv., 2019, 9, 11627–11633.

[26]         Xingjie Dai, Guanglin Weng, Shuowen Yu, Hui Chen, Jiayan Zhang, Shaobing Cheng, Xiaoying Xu, Weicheng Yuan, Zhouyu Wang*, Xiaomei Zhang*， One-pot diastereo- and enantioselective hydrosilylation–transacylation of α-acyloxy β-enamino esters，Org. Chem. Front., 2018, 5, 2787-2793.

[27]         Guangyou Jiang, Min Liu, Dongmei Fang, Ping Tan, Min Huang, Taiping Zhou, Zhenju Jiang, Zhihong Xu and Zhouyu Wang*，Base promoted solvent-free four components reaction for the synthesis of 2,2-disubstituted ethyl cyanoacetates: an improvement of the Ramachary reductive coupling/alkylaiton reaction，RSC Adv., 2018, 8, 8961–8964.

[28]         Lingling Yang ^（*）, Xiaobo Ma , Chen Yuan , Yanying He , Ling Li , Sha Fang , Wei Xia ，Tao He, Shan Qian, Zhihong Xu, Guobo Li, Zhouyu Wang*， Discovery of 2-((4,6-dimethylpyrimidin-2-yl)thio)-N-phenylacet- amide derivatives as new potent and selective human sirtuin 2 inhibitors，European Journal of Medicinal Chemistry，2017，134，230-241.

[29]         Guanglin Weng, Xiaobo Ma, Dongmei Fang, Ping Tan, Lijiao Wang, Linlin Yang, Yuanyuan Zhang, Shan Qian and Zhouyu Wang*，Thiourea catalysed reduction of a-keto substituted acrylate compounds using Hantzsch ester as a reducing agent in water，RSC Advances,2017, 7, 22909 – 22912.

[30]         Ling-Ling Yang, Yan-Ying He, Quan-Long Chen, Shan Qian, Zhouyu Wang*. Design, Synthesis of New 9-Substitued Norharmane Derivatives as Potential Sirt5 Inhibitors. Journal of Heterocyclic Chemistry, 2017，54 , 2，1457–1466.

[31]         Tao He，Ronghua Shi，Yimou Gong，Guangyou Jiang，Ming Liu，Shan Qian，Zhouyu Wang*，Base promoted cascade approach for the preparation of reduced Knoevenagel adducts using Hantzsch esters as reducing agent in water，Synlett，2016，27, 1864-1869.

[32]         Shan Qian, Tao He, Wei Wang, Yanying He, Man Zhang, Lingling Yang, Guobo Li, Zhouyu Wang*, Discovery and preliminary structure–activity relationship of 1H-indazoles with promising indoleamine-2,3-dioxygenase 1 (IDO1) inhibition properties, Bioorganic & Medicinal Chemistry, 2016, 24: 6194–6205.

[33]         Shan Qian, Man Zhang, Quanlong Chen, Yanying He, Wei Wang, Zhouyu Wang*  IDO as a drug target for cancer immunotherapy: recent developments in IDO inhibitors discovery. RSC Advances, 2016, 7575-7581.