王洪根(中山大學教授)

王洪根(中山大學教授)

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王洪根,男,博士,中山大學藥學院教授,博士生導師,是中山大學百人計畫二期引進人才。曾入選廣東省高等學校“優秀青年教師培養計畫”、廣東省特支計畫百千萬工程青年拔尖人才和廣東省高等學校“千百十人才培養工程”校級培養對象。現為嶺南有機化學專業委員會委員,廣東省藥學會第十七屆理事會藥物化學專業委員會委員。曾獲中國科學院優秀博士學位論文獎,中國科學院院長獎學金優秀獎,廣州市科技進步二等獎(排名第二)。主要研究領域為有機合成化學、藥物合成化學、天然產物全合成等。

基本介紹

  • 中文名:王洪根
  • 職業:教師
  • 畢業院校:中國科學院
  • 學位/學歷:博士
  • 職務:博士生導師
  • 職稱:教授
人物經歷,研究領域,教授課程,學術成果,發表論文,出版專著,

人物經歷

2011年9月至2013年8月:博士後,德國明斯特大學,合作導師:Prof. Dr. Frank Glorius;
2006年9月至2011年7月:博士,中國科學院廣州生物醫藥與健康研究院,導師:朱強研究員,張健存研究員;
2005年7月至2005年8月:交換生,香港理工大學套用生物及化學科技學系;
2002年9月至2006年7月:理學學士,雙專業:藥學&計算機科學,中山大學藥學院,中山大學計算機科學系。

研究領域

1.活性及多樣性導向的新型有機合成方法學;
2.活性導向的天然產物全合成;
3.基於生物靶標的合理藥物設計、合成與生物活性研究;
4.藥物新型合成工藝研究.

教授課程

有機化學
藥物合成策略與實例
大學化學實驗

學術成果

發表論文

  1. Tan, D.-H.; Cai, Y.-H.; Zeng, Y.-F.; Lv, W.-X. Yang, L.; Li, Q.; Wang, H.* “Diversity-Oriented Synthesis of α-Functionalized Acylborons and Borylated Heteroarenes via Nucleophilic Ring-Opening of a-Chloroepoxyboronates”Angew. Chem. Int. Ed. 2019, DOI: 10.1002/anie.201907349.
  2. Li, J.; Lin. E.; Han, X.-L.; Li, Q.;* Wang, H.* “Synthesis of Fluorinated Imides via Direct Fluorohydroxylation of Ynamides”, Org. Lett. 2019, 21, 4255-4258.
  3. Lin, E. E.; Wu, J.-Q.; Schäfers, F.; Su, X.-X.; Wang, K.-F.; Li, J.-L.; Chen, Y.; Zhao, X.; Ti, H.; Li, Q.; Ou, T.-M.; Glorius, F.;* Wang, H.* Commun. Chem. 2019, DOI : 10.1038/s42004-019-0137-0
  4. Liu, Y.; Wang H.* “Unified Enantioselective Total Syntheses of (-)-Scholarisine G, (+)-Melodinine E, (-)-Leuconoxine and (-)-Mersicarpine” Chem. Commun. 2019, 55, 3544-3547.
  5. Lv, W.-X.; Li, Z.; Lin, E; Li, J.-L.; Tan, D.-H.; Cai, Y.-H.; Li, Q.; Wang, H. “Regio- and Diastereoselective Synthesis of Cyclohexadienylborons via an Intermolecular Diels-Alder Reaction of Alkenyl MIDA Boronates with 2-Pyrones” Chem. Eur. J. 2019, 25, 4058.
  6. Zhou, C.-J.; Gao, H.; Huang, S.-L.; Zhang, S.-S.; Wu, J.-Q.; Li, B.; Jiang, X.*; Wang, H.* “Synthesis of Benzofused N-Heterocycles via Rh(III)-Catalyzed Direct Benzannulation with 1,3-Dienes” ACS Catal. 2019, 9, 556−564.
  7. Lv, W.-X.; Li, Q.; Li, J.-L.; Li, Z.; Lin, E.; Tan, D.-H.; Cai, Y.-H.; Fan, W.-X.; Wang, H.* “Migratory gem-Difluorination of Alkenyl MIDA Boronates: Facile Synthesis of α- and β-Difluorinated Alkylborons”, Angew. Chem. Int. Ed. 2018, 57, 16544-16548.
  8. Liu, X.-G.; Zhou, C.-J.; Lin, E; Han, X.-L.; Zhang, S.-S.; Li Q.; Wang, H.* “Decarboxylative Negishi Coupling of Redox-Active Aliphatic Ester with Cobalt Catalysis”, Angew. Chem. Int. Ed. 2018, 57, 13096-13100.
  9. Yang, L.; Fan, W.-X.; Lin, E.; Tan, D.-H.; Li Q.; Wang, H.* “Synthesis of α-CF3 and α-CF2H Amines via Aminofluorination of Fluorinated Alkenes”, Chem. Commun. 2018. 54, 5907-5910.
  10. Wang, H.;* Zeng, Y.-F.; Lv W.-X.; Tan D.-H. “Synthetic Transformations of Alkenyl MIDA Boronates toward the Efficient Construction of Organoborons”, Synlett 2018, 29, 1415-1420. (invited Synpacts contribution)
  11. Yang, L.;‡ Ji, W.-W.;‡ Lin, E; Li, J.-L.; Fan, W.-X. Li, Q.; Wang, H.* “Synthesis of Alkylated Monofluoroalkenes via Fe-catalyzed Defluorinative Cross-Coupling of Donor Alkenes with gem-Difluoroalkenes” Org. Lett. 2018, 20, 1924–1927.
  12. Tan, D. H.; Lin, E.; Ji, W.-W.; Zeng, Y.-F.; Fan, W.-X.; Li, Q.; Gao, H.;* Wang, H.* “Copper-Catalyzed Stereoselective Defluorinative Borylation and Silylation of gem-Difluoroalkenes” Adv. Syn. Catal. 2018, 360, 1032-1037.
  13. Zeng, Y.-F.; Ji, W.-W.; Lv, W.-X.; Chen, Y.; Tan, D.-H.; Li, Q.; Wang, H.* “Stereoselective Direct Chlorination of Alkenyl MIDA Boronates: Divergent Synthesis of E and Z α-Chloroalkenyl Boronates” Angew. Chem. Int. Ed. 2017, 56, 14707-14711.
  14. Chen, S.-Y.; Li, Q.;* Wang, H.* “Manganese(I)-Catalyzed Direct C–H Allylation of Arenes with Allenes” J. Org. Chem. 2017, 82, 11173−11181.
  15. Zhang, S.-S.; Xia, J.; Wu, J.-Q.; Liu, X.-G.; Zhou, C.-J.; Li. Q.; Huang, S.-L.;* Wang, H.* “Three-Component Catalytic Carboxygenation of Activated Alkenes Enabled by Bimetallic Rh(III)/Cu(II) Catalysis” Org. Lett. 2017, 19, 5868−5871.
  16. Liu, X.-G.; Gao, H.; Zhang, S.-S.; Li, Q.; Wang, H.* "N-O Bond as External Oxidant in Group 9 Cp*M(III)-Catalyzed Oxidative C−H Coupling Reactions" ACS Catal. 2017, 7, 5078-5086.
  17. Chen, S.-Y.; Han, X.-L.; Li, Q.;* Chen, Y.; Wang, H.* “Mn(I)-Catalyzed Regio- and Stereoselective 1,2-Diheteroarylation of Allenes via a C-H Activation/Directing Group Migration Cascade” Angew. Chem. Int. Ed. 2017, 56, 9939-9943. (Highlighted in Chin. J. Org. Chem. 2017, 37, 2783-2784.)
  18. Ji, W.-W.; Lin, E.; Li, Q.; Wang, H.* “Heteroannulation enabled by a bimetallic Rh(III)/Ag(I) relay catalysis: application in the total synthesis of aristolactam BII” Chem. Commun., 2017, 53, 5665 – 5668.
  19. Chen, S.-Y.; Li, Q.;*Liu, X.-G.; Wu, J.-Q.; Zhang, S.-S.; Wang, H.* “Polycyclization Enabled by Relay Catalysis: One-Pot Manganese-Catalyzed C-H Allylation and Silver-Catalyzed Povarov Reaction” ChemSusChem, 2017, 10, 2360-2364.
  20. Liu, X.-G.; Li, Q.; Wang, H.* “(Pentamethylcyclopentadienyl)cobalt(III)-Catalyzed Direct Trifluoromethylthiolation of Arenes via C-H Activation” Adv. Synth. Catal., 2017, 359, 1942-1946.
  21. Wu, J.-Q.; Zhang, S.-S.; Gao, H.; Qi, Z.; Zhou, C.-J.; Ji, W.-W.; Liu, Y.; Chen, Y.; Li, Q.; Li, X.;* Wang, H.* “Experimental and Theoretical Studies on Rhodium-Catalyzed Coupling of Benzamides with 2,2-Difluorovinyl Tosylate: Diverse Synthesis of Fluorinated Heterocycles” J. Am. Chem. Soc. 2017, 139, 3537-3545.
  22. Tan, D.-H.; Zeng, Y.-F.; Liu, Y.; Lv, W.-X.; Li, Q.; Wang, H.* “Direct Assembly of Prenylated Heteroarenes through a Cascade Minisci Reaction/Dehydration Sequence” ChemistryOpen 2016, 5, 535–539.
  23. Liu, Y.; Zhou, C.-J.; Li, Q.;* Wang, H.* “Total synthesis of (±)-ganocins B and C” Org. Biomol. Chem. 2016, 14, 10362-10365.
  24. Lv, W.-X.;‡ Zeng, Y.-F.;‡ Li, Q.; Chen, Y.; Tan, D.-H.; Yang, L.; Wang, H.* “Oxidative Difunctionalization of Alkenyl MIDA Boronates: A Versatile Platform to Halogenated and Trifluoromethylated α-Boryl Ketones” Angew. Chem. Int. Ed. 2016, 55, 10069-10073.
  25. Lao, Y.-X.; Zhang, S.-S.; Liu, X.-G.; Jiang, C.-Y.; Wu, J.-Q.; Chen, S.-Y.; Li, Q.; Huang, Z.-S.; Wang, H.* “High-Valent Cp*Co(III) or Cp*Ir(III)-Catalyzed C–H Annulation with Alkynes: Straightforward Synthesis of Heterocyclic Quaternary Ammonium Salts. Adv. Synth. Catal., 2016, 358, 2186-2191.
  26. Zhang, S.-S.; Liu, X.-G.; Chen, S.-Y.; Tan, D.-H.; Jiang, C.-Y.; Wu, J.-Q.; Li, Q.*; Wang, H.* “(Pentamethylcyclopentadienyl)cobalt(III)-Catalyzed Oxidative [4+2] Annulation of N-H Imines with Alkynes: Straightforward Synthesis of Multisubstituted Isoquinolines” Adv. Synth. Catal., 2016, 358, 1705-1710.
  27. Liu, X.-G.; Zhang, S.-S.; Jiang, C.-Y.; Wu, J.-Q.; Li, Q.; Wang, H.* “Cp*Co(III)-Catalyzed Annulations of 2-Alkenylphenols with CO: Mild Access to Coumarin Derivatives” Org. Lett., 2015, 17, 5404–5407.
  28. Zhang, S.-S.;‡ Jiang, C.-Y.;‡ Wu, J.-Q.; Liu, X.-G.; Li, Q.; Huang, Z.-S.; Li, D.;* Wang, H.* “Cp*Rh(III) and Cp*Ir(III)-catalysed redox-neutral C–H arylation with quinone diazides: quick and facile synthesis of arylated phenols”, Chem. Commun., 2015, 51, 10240-10243.
  29. Lao, Y.-X.; Wu, J.-Q.; Chen, Y.; Zhang, S.-S.; Li, Q.; Wang H.* “Palladium-catalyzed methylene C(sp3)–H arylation of the adamantyl scaffold”, Org. Chem. Front., 2015, 2, 1374-1378. (From themed collection 2015 Emerging Investigators by OCF, Hot Articles in August and September)
  30. Zeng, Y.-F.; Tan, D.-H. Y.; Chen, Y.; Lv, W.-X.;Liu, X.-G.; Li , Q.; Wang, H.* “Direct Radical Trifluoromethylthiolation and Thiocyanation of Aryl Alkynoate Esters: Mild and Facile Synthesis of 3-Trifluoromethylthiolated and 3-Thiocyanated Coumarins”, Org. Chem. Front., 2015, 2, 1511–1515.
  31. Wu, J.-Q.;, Yang, Z.; Zhang, S.-S.; Jiang, C.-Y.; Li, Q.; Huang, Z.-S.; * Wang H.* “From Indoles to Carbazoles: Tandem Cp*Rh(III)-Catalyzed C–H Activation/Brønsted Acid-Catalyzed Cyclization Reactions”, ACS Catal., 2015, 5, 6453–6457.
  32. Rao, Y.; Liu, H.; Gao, L.; Yu, H.; Ou, T.-M.; Tan, J.-H.; Huang, S.-L.; Wang, H.; Li, D.; Gu, L.-Q.; Ye, J.-M.; Huang, Z.-S. “Synthesis and Biological Evaluation of Novel Bouchardatine Derivatives as Potential Adipogenesis/Lipogenesis Inhibitors for Antiobesity Treatment”, J. Med. Chem., 2015, 58, 9395–9413.
  33. Qiu, J.; Wang, M.; Zhang, Y.; Zeng, P.; Ou, T.-M.; Tan, J.-H.; Huang, S.-L.; An, L.-K.; Wang, H.; Gu, L.-Q.; Huang Z.-S.; Li, D. “Biological Function and Medicinal Research Significance of G-Quadruplex”, Curr. Top. Med. Chem., 2015, 15, 1971-1987
  34. Lv, W.-X.; Zeng, Y.-F. Zhang, S.-S.; Li, Q.; * Wang H.* “Mild Mn(OAc)3-Mediated Aerobic Oxidative Decarboxylative Coupling of Arylboronic Acids and Arylpropiolic Acids: Direct Access to Diaryl 1,2-Diketones”, Org. Lett., 2015, 17, 2972–2975.
  35. Liu, X.-G.; Zhang, S.-S.; Wu, J.-Q.; Li, Q.; Wang H.* “Cp∗Co(III)-catalyzed direct functionalization of aromatic C–H bonds with α-diazomalonates”, Tetrahedron Lett., 2015, 56, 4093-4095.
  36. Zeng, Y.-F.; Tan, D.-H.; Lv, W.-X.; Li, Q.; Wang, H.* “Silver-Catalyzed Aerobic Oxidative Decarboxylative Coupling of Arylpropiolic Acids with H-Phosphine Oxides: Mild and Facile Synthesis of β-Ketophosphine Oxides”, Eur. J. Org. Chem., 2015, 4335–4339
  37. Zhang, S.-S.; Wu, J.-Q.; Liu, X.; Wang, H.* “Tandem Catalysis: Rh(III)-Catalyzed C–H Allylation/Pd(II)-Catalyzed N-Allylation Toward the Synthesis of Vinyl-substituted N-Heterocycles”, ACS Catal. 2015, 5, 210-214.
  38. Wu, J.-Q.; Qiu, Z.-P.; Zhang, S.-S.; Liu, J.-G.; Lao, Y.-X.; Gu, L.-Q.; Huang, Z.-S.*; Li, J.*; Wang, H.* “Rhodium(III)-Catalyzed C–H/C–C Activation Sequence: Vinylcyclopropanes as Versatile Synthons in Direct C–H Allylation Reactions”, Chem. Commun., 2015, 51, 77.
  39. Zhang, S.-S.; Wu, J.-Q.; Lao, Y.-X.; Liu, X.; Liu, Y.; Lv, W.-X.; Tan, D.-H.; Zeng, Y.-F.; Wang, H.* “Mild Rhodium(III)-Catalyzed C-H Allylation with 4-Vinyl-1,3-dioxolan-2-ones: Direct and Stereoselective Synthesis of (E)-Allylic Alcohols”, Org. Lett.,2014,16, 6412–6415.
  40. Cui, W.; Chen, S.; Wu, J.-Q.; Zhao, X.;Hu, W.;H. Wang, “Palladium-Catalyzed Remote C(sp3)–H Arylation of 3-Pinanamine”, Org. Lett.,2014, 16, 4288.
  41. Wang, H.; Beiring, B.; Yu, D.-G.; Collins, K.; Glorius, F. “[3]Dendralene Synthesis: Rhodium(III)-Catalyzed Alkenyl C–H Activation and Coupling Reaction with AllenylCarbinol Carbonate.” Angew. Chem. Int. Ed., 2013, 52, 12430.
  42. Wang, H.; Schröder, N.; Glorius, F. “Mild Rh(III)-Catalyzed Direct C-H Allylation of Arenes with Allyl Carbonates.” Angew. Chem. Int. Ed., 2013, 52, 5386.
  43. Wang, H.; Grohmann, C; Nimphius, C.; Glorius, F.* “Mild Rhodium(III)-Catalyzed C–H Activation and Annulation with Alkyne MIDA Boronates: Short and Efficient Synthesis of Heterocyclic Boronic Acid Derivatives.” J. Am. Chem. Soc., 2012, 134, 19592.
  44. Wang, H.*; Glorius, F.* “Lending Handedness to the Cyclopentadienyl Ligand.” Science, 2012, 338, 479.
  45. Wang, H.; Glorius, F.* “Mild Rhodium(III)Catalyzed C-H Activation and Intermolecular Annulation with Allenes” Angew. Chem. Int. Ed., 2012, 51, 7318.
  46. Wang, H.; Wang, Y.; Liang, D.; Zhang, J.*; Zhu, Q.* “Copper-Catalyzed Intramolecular Dehydrogenative Aminooxygenation: Direct Access to Formyl-Substituted Aromatic N-Heterocycles.” Angew. Chem. Int. Ed.,2011, 50, 5678.
  47. Wang, H.; Wang, Y.; Peng, C.; Zhang, J.*; Zhu, Q.* “A Direct Intramolecular C-H Amination Reaction Cocatalyzed by Copper(II) and Iron(III) as Part of an Efficient Route for the Synthesis of Pyrido[1,2-a]benzimidazoles from N-Aryl-2-aminopyridines.” J. Am. Chem. Soc., 2010, 132, 13217.
  48. Wang, H.; Zhao, J.; Zhang, J.; Zhu, Q.* “BrønstedAcid-Promoted Sequential Hydroarylation-Hydroamidation of Arene Tethered 1-(2-Alkynylphenyl)ureas: Direct Access to 4,4-spiro-3,4-dihydro-2-(1H)-quinazolinones.” Adv. Synth. Catal., 2011, 353, 2653.
  49. Wang, H.; Liu, L.; Wang, Y.; Peng, C.; Zhang, J.*; Zhu, Q.* “An efficient synthesis of 4-alkyl-2(1H)-quinazolinones and 4-alkyl-2-chloroquinazolines from 1-(2-alkynylphenyl)ureas.” Tetrahedron Lett. 2009, 50, 6841-6843.

出版專著

  1. 王洪根,李清江,呂文心,“偕二氟烷基硼酸酯類化合物及其製備方法和套用”,中國專利:申請號,201811174165.5
  2. 王洪根,劉許歌,李清江,“一種丙克拉莫中間體的合成方法”,中國專利:申請號,201810876659.1
  3. 王洪根,周楚鈞,黃世亮,冀衛衛,李清江,“一種苯並稠合N-雜環化合物的製備方法”,中國專利:申請號,2017114647434
  4. 王洪根,勞業興,吳家強,張尚師,“一種金剛烷胺類衍生物及其製備方法和套用”,中國專利:ZL 2015 1 0009169.8
  5. 朱強,王洪根,王勇,梁冬冬,劉蘭英,張健存,“咪唑[1,2-a]吡啶和咪唑醛類化合物的合成方法”中國專利:CN102358739。
  6. 王洪根, 朱強 天然產物全合成薈萃-萜類,第14章,科學出版社,北京,2010.

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