饶燏

饶燏
饶燏 博士生导师 研究员
 

个人简历:       

1995-1999年山东医科大学药学院药物化学专业本科

1999-2002年沈阳药科大学药物化学专业硕士(导师: 陈吉祥教授)

2002-2007年美国佐治亚大学化学系有机化学专业博士 (导师: Prof. Geert-Jan Boons)

2007-2010年美国纪念斯隆-凯特琳癌症中心博士后(导师: Prof. Samuel. J. Danishefsky)

2010-2012 清华大学医学院药学系特别副研究员,博士生导师

2012-至今 清华大学医学院药学系(现药学院)教授, 博士生导师

2014-至今 Editorial Board, ACS Medicinal Chemistry Letters

2014-至今 Editorial Board, Chinese Chemical Letters

主要科研领域及方向:             

  1. 依据蛋白质三维结构进行抗感染疾病, 抗肿瘤小分子化合物的设计,合成与开发;
  2. 发展新型高效的化学方法应用于杂环小分子及片段化合物库的构建及其在抗感染疾病, 抗肿瘤药物研发上的筛选应用;
  3. 具有高生物化性小分子的化学合成及作为分子探针应用于化学生物学研究;

 

实验室研究方向为基于药物发现的化学生物学。通过运用跨学科手段,包括有机合成化学,化学生物学,结构生物学,基因组学和疍白组学等系统生物学技术,围绕基于优势结构‘privileged structure‘的具有潜在高生物学活性的新型小分子化合物的设计,合成与优化及相关靶点,分子信号通路机制研究。寻找新型的,安全,高效的小分子化合物应用于临床转化医学研究。在国际核心期刊(Nature, Angew.Chieme, JACS, Chemical Science, O.L, Chem.Comm, Chem. Eur. J,etc.)上发表论文30余篇。其中有多篇工作被国际专业期刊和网站(OBC, SynFacts, Chin. J. Org. Chem, http://www.organic-chemistry.org)作为亮点工作推荐。为多家国际专业杂志撰写邀请综述文章(包括AsianJOC, Synlett, Tetrahedron)。目前为Angew.Chieme, JACS, Chemical Science,ACS Med Chem Lett,O.L, Chem.Comm, Chem. Eur. J, ChemCatChem, Advanced Synthesis & Catalysis, Asia JOC, 等国际专业杂志审稿人。

代表论文:     

 

  1. Yang, T. Sun, Y. Rao* ‘A Preliminary Study of Diastereoselectivity in Pd(II)-catalyzed C(sp3)-H Alkoxylation of Cyclic system’. , accepted.
  2. Sun, T. Sun, Y. Wu, X. Zhang*, and Y. Rao* ‘A Diversity-Oriented Synthesis of Bioactive Benzanilides by a Regioselective C(sp2)-H Hydroxylation Strategy’. Chemical Science, 2015, DOI: 10.1039/C5SC03905C.
  3. Zhang and Y. Rao.* ” Weak Coordination Promoted Regioselective Oxidative Coupling Reaction for 2,2’-Difunctional Biaryl Synthesis in Hexafluoroisopropanol“. Org. Lett. 2015, 17, 4456-4459 .
  4. Shan, G. Huang, Y. Rao*, H. Zhang*. “Palladium-​catalyzed ortho-​selective C-​H bond chlorination of aromatic ketones“, Chinese Chem. Lett., 2015, 26, Accepted.
  5. Hu, T. Lan, Y. Sun, H. Chen*, J. Yao, and Y. Rao.* ” Unactivated C(sp3)-H Hydroxylation through Palladium Catalysis with H2O as the Oxygen Source “. Chem. Commun., 2015, 51, 14929-14932.
  6. Sun, X. Yao, C. Zhang, and Y. Rao.* ” Palladium Catalyzed ortho C-​H Iodination of Phenylcarbamates at Room Temperature with Cyclic Hypervalent Iodine Reagents “. Chem. Commun., 2015, 51, 10014-10017.
  7. Shan, G. Huang and Y. Rao.* ‘Palladium Catalyzed unactivated β-methylene C(sp3)-H Bond Alkenylation of Aliphatic Amides and Application in A sequential C(sp3)-H/C(sp2)-H Bond Alkenylation’ Org. Biomol. Chem. 2015, 13, 697-701.
  8. Chen, G. Shan, P. Nie and Y. Rao.*.‘3-Alkyloxycyclobutanones as Useful Synthons for Heterocycle and Carbocycle Synthesis’. Asian JOC, 2015, 4, 16-26. (Invited review)
  9. Yang, Z. Chen and Y. Rao.* “Synthesis of Diarylsulfones with Simple Arenes and K2S2O8 through Double C-S Bond Formation “. Chem. Commun., 2014, 50, 15037 -15040.
  10. Zong and Y. Rao.* “Developing Pd(II) catalyzed double sp3 C-H alkoxylation for synthesis of symmetric and unsymmetric acetals”. Org. Lett. 2014, 16, 5278-5281.
  11. Rao*, G. Shan, X. Yang. ‘Some recent advances in transition-metal-catalyzed ortho SP2 C–H functionalization using Ru, Rh, and Pd’, Science China Chemistry, 2014, 57, 930–944. (Invited review)
  12. Yang, Y. Sun, Z. Chen, Y. Rao.* ‘A General Approach towards Catechol and Pyrogallol through Ruthenium and Palladium-Catalyzed C-H Hydroxylation by Weak Coordination’. Adv. Synth. Catal. 2014, 356, 1625-1630.
  13. Sun, Y. Sun, Y. Rao.* ‘A gram-scale synthesis of multi-substituted arenes via palladium catalyzed C-H activation’. Chinese Chem. Lett., 2014, 25, 667-669. (Invited paper)
  14. Hu, H. Xu, P. Nie, X. Xie, Z. Nie* and Y. Rao.* ’ Synthesis of Indazoles and Azaindazoles by Aerobic Oxidative C-N Coupling under Transition Metal Free Conditions’’. , 2014, 20, 3932-3938. (Highlighted by SynFacts 2014, 10(7), 0690)
  15. Sun, Y. Sun, C. Zhang, and Yu Rao.* ’’ Room-Temperature Palladium-Catalyzed C-H Chlorination by Weak Coordination: One-Pot Synthesis of 2-Chlorophenols with Excellent Regioselectivity’’. , 2014, 50, 1262-1264.
  16. Shan, X. Yang, Y. Zong and Y. Rao.* “An Efficient Palladium Catalyzed C-H Alkoxylation of Unactivated Methylene and Methyl Groups with Cyclic Hypervalent Iodine (I3+) Oxidants”. Angew. Chem. Int. Ed. 2013, 52, 13606-13610.
  17. Yang, G. Shan, and Y. Rao.* “Synthesis of 2-Aminophenols and Heterocycles by Ru Catalyzed Mono- and Double C-H Hydroxylation”. Org. Lett. 2013, 15, 2334–2337.
  18. Sun, G. Shan, Y. Sun, and Y. Rao.* “A General Approach for Regio- and Chemoselective C-H Chlorination/Bromination of Electron-Deficient Arenes via Weak Coordination and A Preliminary Study of Priority Order of Relative Directing Group Ability”. Angew. Chem. Int. Ed. 2013, 52, 4440-4444.
  19. Shan, X. Han, Y.Lin, S. Yu,a and Yu Rao.* “Broadening the Catalyst and Reaction Scope of Regio- and Chemoselective C-H Oxygenation: A Convenient and Scalable Approach to 2-Acylphenols by Intriguing Rh(II) and Ru(II) Catalysis “. Org. Biomol. Chem. 2013, 11, 2318-2322. (Highlighted by OBC as a hot article)
  20. Shan, X. Yang, L. Ma, and Y. Rao.* “Pd-Catalyzed C-H Oxygenation with TFA/TFAA: Expedient Access to Oxygen-Containing Heterocycles and Late-Stage Drug Modification”. Angew. Chem. Int. Ed. 2012, 51, 13070-13074. (Highlighted by SYNPACTS and Chin. J. Org. Chem)
  21. Hu, S. Chen, Y. Sun, J. Yang, and Y. Rao.* “Synthesis of Tri- and Tetrasubstituted Pyrazoles via Ru(II) Catalysis: Intramolecular Aerobic Oxidative C–N Coupling”. Org. Lett. 2012, 14, 5030-5033. (Highlighted by SynFacts 2012, 8(12), 1304)
  22. Yang, Y. Lin, and Y. Rao.* “Ruthenium(II)-Catalyzed Synthesis of Hydroxylated Arenes with Ester as an Effective Directing Group”. Org. Lett. 2012, 14, 2874-2877.
  23. Yongfeng Cheng, Xuesong Han, Huangche Ouyang, and Rao.* ’’A New Practical Approach Towards the Synthesis of Unsymmetric and Symmetric 1,10-Phenanthroline Derivatives at Room Temperature’’. , 2012, 48, 2906-2908.
  24. Pengfei Liu, Gang Shan, Shi Chen and Rao.* ‘’A New Regio- and Stereoselective Synthesis of β-Enamino Ketones with 3-Ethoxycyclobutanones and Substituted Amines’’. Tetrahedron Lett. 2012, 53, 936-939.
  25. Shan, X. Sun, Q. Xia and Y. Rao.* “A Facile Synthesis of Substituted 2-Alkylquinolines Through [3+3] Annulation between 3-Ethoxycyclobutanones and Aromatic Amines at Room Temperature”. Org. Lett. 2011, 13, 5770-5773.
  26. Hu, Y. Cheng, Y. Yang and Y. Rao.* “A general and efficient approach to 2H-indazoles and 1H-pyrazoles through copper-catalyzed intramolecular N–N bond formation under mild conditions ”. , 2011, 47, 10133-10135.
  27. Shan, P. Liu and Y. Rao.* “A New Synthesis of Pyrazoles through Lewis Acid-Catalyzed-Union of 3-Ethoxycyclobutanones with Monosubstituted Hydrazines”. Org. Lett. 2011, 13, 1746-1749. 

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