郭海明个人简介

姓   名：

郭海明

职   称：

博士，教授，博士生导师，科技处处长

办公电话：

0373-3329276

电子邮箱：

ghm@htu.edu.cn

个人简介：

郭海明，博士，教授，博士生导师，科技处处长，国家中青年科技创新领军人才，百千万人才工程国家级人选，国家有突出贡献中青年专家，教育部新世纪优秀人才支持计划获得者，河南省学术技术带头人，河南省杰出人才基金获得者，河南省杰出青年基金获得者，河南省青年科技奖获得者，河南创新型科技团队及高校科技创新团队带头人。曾任化学与环境科学学院兼职本科生辅导员，助教，副教授，硕士生导师，教授，博士生导师，副院长，期间，美国Scripps研究所，分子生物学专业，博士后；化学化工学院教授，博士生导师，教务处副处长，博士生导师，科技处处长。主讲课程本科生《波谱分析》，《有机化学及实验》，研究生《不对称合成》，《有机及药物化学专论》。

研究领域：

1.不对称合成；

2.核苷合成方法学研究；

3.分子的荧光标记与荧光识别；

4.核苷类药物的设计与合成。

主要学术及社会兼职：

主持或参加科研项目情况：

1.河南省科技创新杰出人才（164200510008），通过环加成反应合成糖杂核苷类似物，2016.1-2017.12，项目主持人；

2.973计划前期研究专项（2014CB560713），具有抗病毒活性的手性非环核苷类药物的新合成策略研究，2014.10-2016.8，项目主持人；

3.国家自然科学基金（21472037），基于9-联烯嘌呤构建环状大小不同的手性碳环核苷，2015.1-2018.12，项目主持人；

4.国家自然科学基金（21272059），三环及多环核苷的设计、合成及在荧光标记中的应用，2013.1-2016.12，项目主持人；

5.国家自然科学基金（21072047），手性非环核苷类化合物的设计、合成及其药物活性研究，2011.1-2013.12，项目主持人；

6.国家自然科学基金（20802016）, 嘌呤类核苷新化合物的合成及方法学研究, 2009.1-2011.12，项目主持人；

7.高等学校博士学科点专项科研基金（博导类）（20124104110006），“具有荧光活性多环核苷的绿色合成研究”，2013.1-2015.12，项目主持人；

8.教育部新世纪优秀人才支持计划（NCET-09-0122），“冠醚-嘌呤核苷缀合物的合成及其药理活性研究”，2010.1-2012.12，项目主持人；

9河南杰出青年基金（114100510012），“新型手性非环核苷类化合物的设计及合成研究”，2011.1-2013.12，项目主持人；

10.河南省高校科技创新研究团队支持计划(2012IRTSTHN006)：“功能有机分子的设计、合成及活性研究” 2012, 1-2014, 12.团队负责人；

11.河南省科技开放合作项目（132106000068）：“腺苷蛋氨酸的合成及产业化”，2014.1-2015.12，项目主持人；

12.河南省高等教育教学改革研究项目（2009SJGLX145）“化学类专业人才培养方案与课程体系综合改革与实践”，2009.9-2011.9，项目主持人；

13.河南省高等教育教学改革研究项目（）, “分流培养模式下教学质量保障体系的探索与实践”，2012.1-2013.12，项目主持人；

14.新乡市科技创新平台建设项目（），“新型手性非环核苷类药物的设计与合成”，2012-2014，项目主持人；

15.企业横向项目，“三种阿糖核苷的合成方法及产业化研究”，2009.8-2010.8，项目主持人。

16.杰出青年基金，“手性非环核苷的不对称合成”，2011.1-2013.12，项目主持人。

17.国家自然科学基金（20772025），5-取代嘧啶碳环核苷的合成及生物活性研究, 2008.1-2010.12，第3参加人；

18.国家自然科学基金（20772024），脱氧核苷的合成新方法新方法研究, 2008.1-2010.12，第3参加人；

19.国家自然科学基金（29972010），微波技术合成核苷类化合物的新方法研究, 2003.1-2006.12，第5参加人；

20.国家自然科学基金（20472082），手性有机小分子催化剂设计及其在不对催化反应中的应用, 2004.1-2007.12，第4参加人；

21.河南省杰出人才创新基金(074200510020)，绿色合成技术在脱氧及氟代核苷的合成及产业化中的应用研究, 2008.1-2010.12，第3参加人。

学术成果：

代表性论文：

[1] Dong-Chao Wang, Ming-Sheng Xie, Hai-Ming Guo*, Gui-Rong Qu, Meng-Cheng Zhang, Shu-Li   You*, Enantioselective Dearomative [3+2]   Cycloaddition Reactions of Benzothiazoles, Angew. Chem. Int. Ed. 2016, in press.

[2] Dan-Jie Zhang, Ming-Sheng Xie*, Gui-Rong Qu,   Yao-Wei Gao, and Hai-Ming Guo*, Synthesis of Azacyclic Nucleoside   Analogues via Asymmetric [3 + 2] Cycloaddition of 9-(2-Tosylvinyl)-9H-purines,   Org. Lett., 2016, 18(4), 820–823.

[3] Dong-Chao Wang, Hai-Xia Wang, Er-Jun Hao, Xiao-Han   Jiang, Ming-Sheng Xie, Gui-Rong Qu* and Hai-Ming Guo*, Synthesis of 3,3-Disubstituted Oxindoles   Containing a 3-(4-Aminobut-2-ynyl) Unit via Domino Heck–Sonogashira   Reaction in Water, Adv.   Synth. Catal., 2016,   358: 494–499.（as a VIP paper. see Inside cover）

[4] Hua Zhang*, Kui Wang, Xiao-peng Xuan, Qing-zhang Lv, Ya-min Nie, Hai-ming Guo*, Cancer Cells-Targeted Two-Photon   Fluorescence Probe for the Real-time Ratiometric Imaging of DNA Damage,   Chem. Commun., 2016,52, 6308-6311.

[5] Dong-chao Wang, Ran Xia, Ming-sheng Xie, Gui-rong Qu*, Hai-ming Guo*, Synthesis of Cycloalkyl Substituted Purine   Nucleosides via a Metal-Free Radical Route, Org. Biomol. Chem.,   2016, 14, 4189-4193. (Invited paper )

[6] Huan-Li Sun, Fei Chen, Ming-Sheng Xie, Hai-Ming Guo*, Gui-Rong Qu, Yan-Mei He,   Qing-Hua Fan*, Asymmetric Hydrogenation of α-Purine   Nucleobase-Substituted Acrylates with Rhodium Diphosphine Complexes: Access   to Tenofovir Analogues, Org. Lett.,   2016, 18 (9), 2260–2263.

[7] ‍‍‍‍Jianping Li, Yanyan Zhang, Hua Zhang*, Xiaopeng   Xuan, Mingsheng Xie, Shuang Xia, Guirong Qu, Haiming Guo‍‍*, ‍‍Nucleoside-based Ultrasensitive FluorescentProbe for   the Dual-mode Imaging of Microviscosity in Living Cells, Anal.Chem., 2016,   88 (10), 5554–5560.

[8] Hai-Xia Wang, Dan-Dan Xi, Ming-Sheng Xie*, Hui-Xuan Wang,   Gui-Rong Qu, Haiming Guo*Nucleoside-Based Diarylethene   Photoswitches: Synthesis and Photochromic Properties, ChemBioChem,   2016, 17(13), 1216–1220.

[9] Ming-Sheng   Xie, Peng Zhou, Hong-Ying Niu, Gui-Rong Qu*, Hai-Ming   Guo*, Enantioselective Intermolecular   Cyclopropanations for the Synthesis of Chiral Pyrimidine Carbocyclic   Nucleosides, Org. Lett., 2016,   18(17), 4344–4347. (highlighted by Synfacts )

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[10] Peng Zhou, Ming-Sheng Xie, Gui-Rong Qu*, Ren-Long Li, Hai-Ming Guo*, Synthesis of Acyclic Nucleoside Analogues   via the Insertion of Carbenoids into N-H Bond of Nucleobases, Asion   J. Org. Chem. 2016, 5, 1100–1106.

[11]Hui-Li Liu, Ming-Sheng Xie*,   Gui-Rong Qu, and Hai-Ming Guo*, Organocatalytic Enantioselective Allylic   Etherification of Morita–Baylis–Hillman Carbonates and Silanols,   J. Org. Chem., 2016, DOI: 10.1021/acs.joc.6b01931.

[12]Ming-Sheng Xie, Yong Wang, Jian-Ping Li,* Cong Du, Yan-Yan Zhang,   Er-Jun Hao, Yi-Ming Zhang, Gui-Rong Qu, Hai-Ming   Guo* A Straightforward Entry to Chiral   Carbocyclic Nucleoside Analogues via Enantioselective [3+2] Cycloaddition of   -Nucleobase Substituted Acrylates, Chem. Commun.,2015, 51, 12451 -   12454.

[13]Hua Zhang*, Caixia Wang,   Tao Jiang, Haiming Guo*, Ge Wang, Xinhua Cai,   Lin Yang, Yi Zhang, Haichuan Yu, Hui Wang, and Kai Jiang, Microtubule-Targetable Fluorescent Probe:   Site-Specific Detection and Super-Resolution Imaging of Ultratrace Tubulin in   Microtubules of Living Cancer Cells, Anal. Chem., 2015，87 (10),  5216–5222.

[14]Hong-Ying Niu*,Cong Du, Ming-Sheng Xie, Yong Wang, Qian   Zhang,Gui-Rong Qu, and Hai-Ming Guo*,Diversity-Oriented Synthesis of Acyclic   Nucleosides via Ring-Opening of Vinyl Cyclopropanes with Purines, Chem.   Commun.,2015, 15, 3328-3331.

[15]Ming-Sheng Xie, Hong-Ying Niu*, Gui-Rong Qu, and Hai-Ming Guo*，The development for the synthesis of   chiral acyclic nucleosides and their phosphonates,Tetrahedron Letters 55 (2014), pp. 7156-7166.（Invited Digest Paper）

[16]Qi-Liang Yang, Ming-Sheng Xie, Chao Xia, Huan-Li Sun, Dan-Jie   Zhang, Ke-Xin Huang, Zhen Guo, Gui-Rong Qu*, and Hai-Ming Guo*，A rapid and divergent access to chiral   azacyclic nucleoside analogues via highly enantioselective 1,3-dipolar   cycloaddition of β-nucleobase substituted acrylates,Chem. Commun., 2014,50,   14809-14812.

[17]Shao-Hua Gao,Ming-Sheng Xie, Hai-Xia Wang, Hong-Ying Niu, Gui-Rong   Qu,*and Hai-Ming Guo*,Highly Selective Detection of Hg2+   ion by Push-Pull-Type Purine Nucleoside-Based Fluorescent Sensor, Tetrahedron, 2014, 70,   4929-4933.

[18]Qian Zhang*, Bai-Wei Ma, Qian-Qian Wang, Xing-Xing Wang, Xia Hu,   Ming-Sheng Xie, Gui-Rong Qu, and Hai-Ming Guo*,   The Synthesis of Tenofovir and its   Analoguesvia Asymmetric Transfer Hydrogenation,Org. Lett. 2014,16, 2014-2017.

[19]Ren-Long Li, Lei Liang, Ming-Sheng Xie, Gui-Rong Qu,* Hong-Ying   Niu, Hai-Ming Guo,*Copper-Catalyzed Intramolecular   Cyclization of N-Propargyl-Adenine: Synthesis of Purine-Fused PolycyclicsJ.   Org. Chem. 2014,79,   3665-3670.

[20]Jian-Ping Li, Hui-Xuan Wang, Hai-Xia Wang,* Ming-Sheng Xie,   Gui-Rong Qu, Hong-Ying Niu, Hai-Ming Guo,*Push-Pull-Type Purine Nucleoside-Based   Fluorescent Sensors for the Selective Detection of Pd2+ in Aqueous   Buffer,Eur. J. Org. Chem.2014,   2225-2230.  

[21]Qian Zhang,* Yong-Zhen Huang, Jun-Hui Yang, Bai-Wei Ma, Gui-Rong   Qu, Hai-Ming Guo,* Synthesis of 9-oxiranyl-9H-purine   derivatives in β-cyclodextrin cavity, Tetrahedron Letters2014, 55, 1203-1206.

[22]Ming-Sheng Xie; Zhi-Liang, Chu, Hong-Ying Niu, Gui-Rong Qu,* Hai-Ming Guo*, A Copper-Catalyzed Domino Route toward   Purine-Fused Tricyclic Derivatives, J. Org. Chem.2014, 79, 1093-1099.

[23] Tao Wei, Ming-Sheng Xie, Gui-Rong Qu,* Hong-Ying Niu, and Hai-Ming Guo*, A New Strategy to Construct Acyclic   Nucleosides via Ag(I)-Catalyzed Addition of Pronucleophiles to   9-Allenyl-9H-Purines,Org. Lett.2014, 16, 900-903.

[24]Ran Xia, Ming-Sheng Xie, Hong-Ying Niu, Gui-Rong Qu,* and Hai-Ming Guo*, Efficient synthesis of nebularine and   vidarabine via dehydrazination of (hetero)aromatics catalyzed by CuSO4   in water,Green Chem.2014, 16, 1077-1081.

[25]Ran Xia, Ming-Sheng Xie, Hong-Ying Niu, Gui-Rong Qu,* and Hai-Ming Guo,* Radical Route for the Alkylation of Purine   Nucleosides at C6 via Minisci Reaction,Org. Lett.2014,   16, 444-447.

[26] Dong-Chao Wang, Hong-Ying Niu, Ming-Sheng Xie,   Gui-Rong Qu,* Hui-Xuan Wang, and Hai-Ming Guo,*Highly Regioselective Three-Component   Domino Heck−Negishi Coupling Reaction for the Functionalization of Purines at   C6,Org. Lett.2014, 16, 262-265.

[27].Jian-Ping Li, Yu Huang, Ming-Sheng Xie,Gui-Rong   Qu, Hong-Ying Niu,* Hai-Xia Wang, Bo-Wen Qin, and Hai-Ming Guo,* One-Pot Synthesis of   7,9-Dialkyl-Purin-8-One Analogues: Broad Substrate Scope, J. Org.   Chem. 2013, 78, 12629-12636.(Highlighted by JOC Homepage)

[28]Hai-Ming Guo,* Run-Ze Mao, Qiao-Tian Wang, Hong-Ying   Niu,Ming-Sheng Xie,and Gui-Rong Qu* , Pd(II)-Catalyzed One-Pot, Three-Step route for the   Synthesis of Unsymmetrical Acridines, Org. Lett.2013, 15, 5460-5463.

[29].Qian Zhang,* Bai-Wei Ma, Yong-Zhen Huang, Qian-Qian   Wang, Xing-Xing Wang, Gui-Rong Qu, and Hai-Ming Guo*Efficient Synthesis of Purine Derivatives by one-pot three-component mannich type  reaction,Heterocyclics, 2013,   87, 2081-2091.

[30]Jia-jia Jin, Dong-chao Wang, Hong-ying Niu*, Shan Wu, Gui-rong Qu,   Zhong-bo Zhang and Hai-Ming Guo*,Brønsted Acid Catalyzed Synthesis of   1,3-Di(2-quinolyl)propane Derivatives via Tandem C(sp3)-H   Functionalization, Tetrahedron, 2013, 69, 6579-6584.

[31] Qian Zhang*, Gang Cheng, Yong-Zhen Huang, Gui-Rong Qu, Hong-Ying   Niu, Hai-Ming Guo*, Regioselective N9 alkylation of purine   rings assisted by b-cyclodextrin, Tetrahedron, 2012, 68, 7822-7826.

[32] Ran Xia, Hong-Ying Niu, Gui-Rong Qu,* Hai-Ming Guo*, CuI Controlled C-C and C-N Bond Formation   of Heteroaromatics through C(sp3)-H Activation, Org. Lett.,2012, 14, 5546–5549.(Highlighted by SYNFACTS, 2013, 2(9), 0197.and   Org. Chem. Portal.)

[33] Hong-Ying Niu, Shi-Xia Bai, Shan Wu, Gui-Rong Qu,* Hai-Ming Guo*, Synthesis of Chiral N-(Purin-6-yl)amino   Acids Derivatives: Using Natural Amino Acids as Starting Materials, Asian   J. Org. Chem., 2012, 1, 238–244.

[34] Gui-Rong Qu, Lei Liang, Hong-Ying Niu, Wei-Hao Rao, Hai-Ming Guo,* John S. Fossey,* Copper-Catalysed Synthesis of Purine-Fused   Polycyclics, Org. Lett., 2012,14(17),4494–4497.

[35]. Jin-Ying Liu,Hong-Ying Niu,Shan Wu, Gui-Rong Qu,* Hai-Ming Guo,*Metal Catalyzed C(sp3)-H Bond   Amination of 2-Alkyl Azaarenes with Diethyl Azodicarboxylate, Chem.   Commun., 2012, 48 (78),   9723-9725.(Top ten most accessed articles in August)

[36]Ge Meng, Hong-Ying Niu, Gui-Rong Qu, John S. Fossey, Jian-Ping Li,*   Hai-Ming Guo,* 'Synthesis of Fused N-Heterocycles via   Tandem C-H Activation' Chem. Commun.,2012, 48, 9601-9603. (Top ten most accessed articles in July)

[37] Peng-Yang Xin, Hong-Ying Niu, Gui-Rong Qu,* Rui-Fang Ding, Hai-Ming Guo*, Nickel catalyzed alkylation of N-aromatic   heterocycles with Grignard reagents through direct C-H bond functionalization,   Chem. Commun.,2012, 48,   6717-6719. (Highlighted by SYNFACTS, 2012, 8(8), 0901.)

[38] Jia-Jia Jin, Hong-Ying Niu, Gui-Rong Qu, Hai-Ming Guo,* John S. Fossey*, Copper-catalysed addition of a-alkyl   azaarenes to ethyl glyoxylate via direct C(sp3)-H activation,   RSC Adv., 2012, 2, 5968-5971 .

[39] Gui-Rong Qu,* Yan-Wei Song, Hong-Ying Niu, Hai-Ming Guo,* John S. Fossey,Cu(OTf)2-catalyzed Ritter   reaction: Efficient synthesis of amides from nitriles and halohydrocarbons in   water, RSC Adv., 2012, 2, 6161-6163 . (Highlighted   by Chemistry in Water of Organic & Biomolecular   Chemistry Blog, 2014-3-20至2014-4-21)

[40]. Gui-Rong Qu,* Hong-Liang Zhang, Hong-Ying Niu, Zai-Kun Xue,   Xin-Xin Lv, Hai-Ming Guo*, Synthesis of C6-Azolyl Purine Nucleosides   via C-N Coupling Reaction of Unprotected 6-Chloropurine Nucleosides and   N-Heterocycles under Catalyst- and Solvent-Free Conditions, Green   Chem.,2012, 14, 1877-1879 .

[41] Hong-Ying Niu, Chao Xia, Gui-Rong Qu*, Shan Wu, Yi   Jiang, Xin Jin, Hai-Ming Guo*Microwave Promoted One-Pot Synthesis of   4-Nitrobenzylthioinosine Analogues Using Thiourea as a Sulfur Precursor,   Chemistry - An Asian Journal, 2012, 7(1), 45-49.

专利成果：

1. 化学合成法生产腺苷的工艺，(ZL01127525.1)，授权时间2005.1.26；(第6完成人)

2. 化学合成法生产2,6-二氯嘌呤核苷的工艺，(ZL200710053919.7)，授权时间2009.1.26；(第3完成人)

3. 化学合成法生产胞苷的工艺，(ZL200710053853.1)，授权时间2009.5.3。(第5完成人)

4. 具有抗癌活性的6-位被单氮杂冠醚修饰的嘌呤核苷类新化合物及制备方法，（ZL 2009 1 0064796.6），授权时间2010.12.9，(第1完成人)

5. 5-环己基阿糖尿苷、制备方法及其应用，（ZL201310428434.7），授权时间2015.05.27，(第2完成人)

6. 8-环己基-2-氟阿糖腺苷、制备方法及其应用,（ZL201310428421.X），授权时间2015.05.27，(第1完成人)