- 马小锋
- 电子邮件:maxf@cib.ac.cn
- 职 称:研究员
- 学 历:博士研究生
- 通讯地址:四川省成都市天府新区群贤南街23号
- 邮 编:610213
个人简历
中国科学院成都生物研究所研究员,博士生导师。中科院BR计划,四川省QR计划获得者。以发展绿色、高效、高选择性新合成方法为核心,以从廉价易得的原料精准创制具有丰富生物学功能的高附加值化学品为主要使命。围绕杂环类化合物多样性导向的合成与转化,发展新反应、新试剂,并探索所得化合物的新功能,以期开发具有自主知识产权的药物、农药。主要贡献包括:(1) 实现了光促进的亚砜的Thia-Baeyer-Villiger氧化重排反应,证明了氧原子插入亚砜键的可能性,并利用该反应成功实现了生物模拟催化脱硫过程;(2) 提出并验证了两个反应中间体可以形成电子给体-受体复合物 (EDA复合物),并激发后续串联反应,发展了氮杂环合成及多样性转化新方法。(3) 发展了高效、高选择性糖的官能团修饰策略,为活性糖苷类药物分子的经济高效获取提供了新途径。围绕上述研究,以第一或通讯(含共同)在Nat. Commun.、J. Am. Chem. Soc.、Angew. Chem. Int. Ed.,JACS Au、Green Chem.等国际重要学术期刊发表论文30余篇,申请中国发明专利7项,已授权2项。
教育经历:
2003.09—2007.07 兰州大学,药学院,药学专业,医学学士
2007.09—2012.07 中国科学院成都生物研究所,天然产物研究中心,药物化学,理学博士(导师:邵华武研究员)
2007.09—2008.07 中国科学技术大学化学系(理论课程学习)
工作经历:
2012.07—2012.10中国科学院成都生物研究所天然产物研究中心,研究助理(项目聘用)
2012.12—2016.03比利时法语鲁汶大学有机化学和药物化学系 (合作导师: Istv n E. Mark 教授),博士后
2016.03—2019.03英国布里斯托大学化学系(合作导师:John. F. Bower 教授),博士后
2019.08—至今 中国科学院成都生物研究所,研究员
研究方向
糖化学、有机合成、药物化学、不对称合成
社会任职
获奖及荣誉
中国科学院BR计划、四川省QR计划、四川省特聘专家
承担科研项目情况
1. 中国科学院BR计划项目,300万,2022.01.11-2025.01.10,在研,主持.
2. 苷类化合物库建立及药物先导化合物发现,中国科学院科技促进发展局,战略生物资源服务网络计划“活性天然产物发现、评估与转化平台”项目 (子项目, KFJ-BRP-008-002),300万,2021.11.23- 2024.10.31,在研,主持.
1,3-双吲哚糖衍生物的合成及活性评估,国家自然科学基金面上项目(22377123),,50万,2024.01-2027.12,在研,主持
4. 高效、高选择性酰基糖C-苷的合成研究,四川省科技厅中央引导地方项目(2022ZYD0047),40万,2022.08-2023.08,在研,主持.
5. 分子内不对称去芳香化C-N键形成及其串联反应,国家自然科学基金青年项目(22001246),24万,2021.01.01- 2023.12.31,结题,主持.
6. 糖C-苷类化合物的合成研究,四川省QR计划项目,50万,2020.12.27-2022.12.31,结题,主持
代表论著
代表性论文:
1.Jiangtao Li, Zhengyan Fu, Zeen Qiao, Demeng Xie, Li Zhang, Ya-Zhou Liu, Jian Yang, Jia-Xin Yan,Xiaofeng Ma,* Controllable 1,3-bis-Functionalizaiton of 2-Nitroglycals with High Regioselectivity and Stereoselectivity Enabled by a H-Bond Catalyst, JACS Au 2024, 4, 974−984.
2. Li Zhang, Wei Zeng, Demeng Xie, Jiangtao Li, Xiaofeng Ma,* Nickel and Chiral Phosphoric Acid Cocatalysis Enables Synthesis of C-Acyl Glycosides, Org. Lett. 2024, 26, 1332−1337.
3. Ya-Zhou Liu, Yu Chen, Amu Wang, Zhongke Shen, Xueting Zhou, Jichao Zhang, Yinxiang Jian, Xiaofeng Ma,* Electron-donor-acceptor Complex Between Two Intermediates Enables a N-N Bond Cleavage Cascade Process to Access 2,3-Difunctionalized Pyridines, Green Chem. 2024, 26, 2280–2289.
4. Yong-Qiang Wang,* Wei-Ting Chen, Xia Liu, Hua Zhu, Xuan Qiao, Yuzhi Wang, Xiaofeng Ma,* Development of a Safe, Efficient and Scalable Process for the Synthesis of Midazolam Hydrochloride, Org. Process Res. Dev. 2023, 27, 2374–2384.
5. Xiaofang Hu, Zeen Qiao, Li Zhang, Jinzhong Zhao, Ya-Zhou Liu, Jiangang Zhang,* Xiaofeng Ma,* One-pot Cascade Synthesis of Dibenzothiophene-based Heterobiaryls from Dibenzothiophene-5-oxide, Org. Biomol. Chem. 2023, 21, 9123–9127.
6. Junxiu Liang, Ya-Zhou Liu, Amu Wang, Yanchao Wu, Xiaofeng Ma*, Huijing Li*, Dearomatization of Halonaphthols via an Intermolecular [4+1] Spiroannulation with in situ Formed Aza-Ortho-Quinone Methides, Chin. J. Org. Chem. 2023, 43,3888–3899.
7. Jian Yang, Shanqiao Wei, Jinzhong Zhao, Wei Zeng, Huawu Shao*, Xiaofeng Ma*, An Environmentally Benign Protocol for the Synthesis of Sugar 1,2-Orthoesters in Poly(ethylene glycol) Dimethyl Ether (DMPE), Carbohydr. Res. 2023, 534, 108902.
8. Hailong Shi, Jinlian Yang, Zeen Qiao, Lingyu Li, Gang Liu, Qi Dai, Li Xu, Wei Jiao, Guolin Zhang, Fei Wang, Xiaoxia Lu*, Xiaofeng Ma*, Design, Synthesis and Structure–Activity Relationship Studies on Erianin Analogues as Pyruvate Carboxylase (PC) Inhibitors Against Hepatocellular Carcinoma Cells, Org. Biomol. Chem. 2023, 21, 7005-7017.
9. Jian Yang, Demeng Xie, Xiaofeng Ma*, Recent Advances in Chemical Synthesis of Amino Sugars, Molecules, 2023, 28, 4724.
10. Yinxiang Jian, Peng Liang, Xiaoyan Li, Huawu Shao*, Xiaofeng Ma*, Controllable Transformation of Indoles Using Iodine(III) Reagent, Org. Biomol. Chem. 2023, 21, 179-186.
11. Xiaoke Zhang, Ya-Zhou Liu, Huawu Shao*, Xiaofeng Ma*, Advances in Atroposelectively De Novo Synthesis of Axially Chiral Heterobiaryl Scaffolds Molecules 2022, 27, 8517.
12. Hailong Shi, Jian Yang, Yao Cheng, Jinlian Yang, Xiaoxia Lu*, Xiaofeng Ma*, 1, 2-trans-Stereoselective 7-O-Glycosylation of Flavonoids with Unprotected Pyranoses by Mitsunobu Reaction, Chem. Asian J. 2022, 17, e2022001.
13. Zhongke Shen, Qin Tang, Wei Jiao, Huawu Shao*, Xiaofeng Ma*, One-Pot Synthesis of 2-C-Branched Glycosyl Triazoles by Integrating 1,2-Cyclopropanated Sugar Ring-Opening Azidation and CuAAC Reaction, J. Org. Chem. 2022, 87, 16736-16742.
14. Amu Wang, Ya-Zhou Liu,Zhongke Shen, Zeen Qiao, Xiaofeng Ma*, Regioselective Synthesis of Pyrazolo[1,5-a]pyridine via TEMPO Mediated [3+2] Annulation-Aromatization of N-Aminopyridines and , -Unsaturated Compounds, Org. Lett. 2022, 24, 7, 1454-1459.
15. Peng Liang, Hang Zhao, Tingting Zhou, Kaiyun Zeng, Wei Jiao, Yang Pan, Yazhou Liu, Dongmei Fang, Xiaofeng Ma*, Huawu Shao*. Rapid Oxidation Indoles into 2-Oxindoles Mediated by PIFA in Combination with n-Bu4NCl H2O, Adv. Synth. Catal. 2021, 363, 3532-3538.
16.Xiaofeng Ma*, Yazhou Liu, Le Du, Jingwei Zhou, Istv n E. Mark . Post-functionalization of Dibenzothiophene to Functionalized Biphenyls via a Photoinduced Thia-Baeyer-Villiger Oxidation, Nat. Commun. 2020, 11, 914.
17. Xiaofeng Ma, Ian R. Hazelden, Thomas Langer, Rachel H. Munday, John F. Bower*. Enantioselective Aza-Heck Cyclizations of N‑(Tosyloxy)carbamates: Synthesis of Pyrrolidines and Piperidines, J. Am. Chem. Soc. 2019, 141, 3356-3360. (Highlight in Synfacts, 2019; 15, 0483).
18. Xiaofeng Ma, Joshua J. Farndon, Tom A. Young, Natalie Fey, John F. Bower*, A Simple and Broadly Applicable C-N Bond Forming Dearomatization Protocol Enabled by Bifunctional Amino-Reagents, Angew. Chem. Int. Ed. 2017, 56, 14531-14535. (Highlight in Org. Process Res. Dev. 2017, 21, 1873-1883).
19. Ian R. Hazelden,+ Xiaofeng Ma,+(+并列第一作者) Thomas Langer, John F. Bower*, Diverse N-Heterocyclic Ring Systems via Aza-Heck Cyclizations of N-(Pentafluorobenzoyloxy)sulfonamides, Angew. Chem. Int. Ed. 2016, 55, 11198-11202.
20.Xiaofeng Ma,* Damien F. Dewez, Le Du, Xiya Luo, Istv n E. Mark , Kevin Lam*, Synthesis of Diketones, Ketoesters and Tetraketones by Electrochemical Oxidative Decarboxylation of Malonic Acid Derivatives: Application to the Synthesis of cis-Jasmone, J. Org. Chem. 2018, 83, 12044-12055.
21. Xiaofeng Ma, Hodney Lubin, gnes Simon, Enik Ioja, Orsolya K kesi, gota Ap ti, Tam s I. Orb n, L szl H ja, Julianna Kardos, Istv n E. Mark *, Straightforward and Effective Synthesis of -Aminobutyric Acid Transporter Subtype 2-Selective Acyl-Substituted Azaspiro[4.5]decanes, Bioorg. Med. Chem. Lett. 2016, 26, 417-423.
22. Xiaofeng Ma, Xiya Luo, Simon Dochain, Charlotte Mathot, Istv n E. Mark *, Electrochemical Oxidative Decarboxylation of Malonic Acid Derivatives: A Method for the Synthesis of Ketals and Ketones, Org. Lett.2015, 17, 4690-4693. (Featured on Organic Chemistry Portal, https://www.organic- chemistry. org/ abstracts /lit5/128.shtm)
23. Xiaofeng Ma, Jichao Zhang, Qin Tang, Jun Ke, Wei Zou, Huawu Shao*, Stereospecific [3+2] Cycloaddition of 1,2-Cyclopropanated Sugars and Ketones Catalyzed by SnCl4: an Efficient Synthesis of Multi-Substituted Perhydrofuro[2,3-b]furans and Perhydrofuro[2,3-b]pyrans,Chem. Commun. 2014, 50, 3505-3508.
24. Xiaofeng Ma, Qin Tang, Jun Ke, Jichao Zhang, Xinglong Yang, Xudong Shen, Huawu Shao*, A Neighboring Group Participation Strategy: Direct and Highly Diastereoselective Synthesisof 2-Substituted and 2,2-Bisubstituted Perhydrofuro[2,3-b]pyran Derivatives, Org. Biomol. Chem. 2014, 12, 7381-7388.
25. Xiaofeng Ma, Qin Tang, Jun Ke, Jichao Zhang, Cong Wang, Haibo Wang, Yuxue Li, Huawu Shao*, Straightforward and Highly Diastereoselective Synthesis of 2,2-Disubstituted Perhydrofuro[2,3-b]pyran (and furan) Derivatives Promoted by BiCl3, Chem. Commun. 2013, 49, 7085-7087 (Highlight in Synfacts, 2013; 9, 1212).
26. Xiaofeng Ma, Qin Tang, Jun Ke, Xinglong Yang, Jichao Zhang, Huawu Shao*, InCl3 Catalyzed Highly Diastereoselective [3+2] Cycloaddition of 1,2-Cyclopropanated Sugars with Aldehydes: a Straightforward Synthesis of Persubstituted Bis-Tetrahydrofurans and perhydrofuro [2,3-b]pyrans,Org. Lett. 2013, 15, 5170-5173.
27. Xiaofeng Ma, Qin Tang, Jun Ke, Haibo Wang, Wei Zou, Huawu Shao*, A Convenient and Highly Stereoselective Method for Synthesis of Octahydropyrano[3,2-b]pyrrole Derivatives, Carbohydr. Res. 2013, 366, 55-62.
28. Shuaibing Zhang, + Xiaofeng Ma, + (+并列第一作者) Xiaoqiong Pei, Jingyuan Liu, Huawu Shao, Zhongliu Wu, A Practical High-throughput Screening System for Feruloyl Esterases: Substrate Design and Evaluation,J. Mol. Catal.B-Enzym. 2012, 74, 36-40.
29. Xiaofeng Ma, Qiang Tian, Qin Tang, Huawu Shao*, A Novel and Highly Stereoselective Synthesis of 2-Substituted Perhydrofuro[2,3-b]pyran Derivatives, Org. Lett. 2011, 13, 4276-4279.
代表性专利:
1. 马小锋,李江涛,一种3-吲哚或吡咯基-2-硝基烯糖类化合物及其制备方法与应用,专利申请号: 202410059158.X
2. 马小锋,李江涛,一种2-硝基-2-烯吲哚糖碳苷类化合物及其合成方法与应用,专利申请号: 202310766858.8
3. 马小锋,李江涛,付征雁,一种吲哚糖碳苷类大环化合物及其制备方法与应用,专利申请号: 202310691698.5
4. 马小锋,刘亚洲,王阿木,一种4-氮杂吲哚啉类化合物及其合成方法与应用,专利申请号:202310032248.5.
5. 马小锋,李江涛,吲哚糖苷类化合物及吡咯糖苷类化合物及合成方法与应用。专利申请号:202211581675.0.
6. 马小锋,刘亚洲,王阿木,史小可,王飞,调节雌激素受体合成活性的吡唑并吡啶衍生物,专利号:ZL202110786668.3.
7. 马小锋,刘亚洲,一种二苯并[c,e][1,2]氧硫杂环己烷-6-氧化物类化合物的转化方法,专利号:ZL201910893751.3.
代表性论著(章节):
1. 黄胜雄、马小锋、尹文斌、青琳森、周燕、卿立燕,中国生物经济发展报告2023,生物资源保护利用发展现状与趋势(第28章),国家发展和改革委员会创新和高技术发展司,国家发展和改革委员会创新驱动发展中心(数字经济研究发展中心),中国生物工程学会。