Zhai Group
School of Chemical Biology & Biotechnology


82. Xu, B; Xun, W; Su, S; Zhai, H.* Total Syntheses of (–)-Conidiogenone B, (–)-Conidiogenone and (–)-Conidiogenol, Angew. Chem. Int. Ed. 2020, 59, 16. DOI: 10.1002/anie.20200724781. Zhao, H.; Wang, T.; Qing, Z.; Zhai, H.* Cobalt-catalyzed 2-(1-methylhydrazinyl)pyridine-assisted cyclization of thiophene-2-carbohydrazides with maleimides: efficient synthesis of thiophene-fused pyridones, Chem. Commun., 2020, 56, 55245527. DOI: 10.1039/d0cc01582b

80. Qiu, S.;  Zhai, S.;  Wang, H.;  Chen, X.; Zhai, H.* One-pot synthesis of benzo b fluorenones via a cobalt-catalyzed MHP-directed 3+2 annulation/ring-opening/dehydration sequence. Chem. Commun. 2019, 55, 42064209. DOI: 10.1039/c9cc00948e

79. Zhao, H.;  Shao, X.;  Qing, Z.;  Wang, T.;  Chen, X.;  Yang, H.; Zhai, H.* Cobalt‐Catalyzed 2‐(1‐Methylhydrazinyl)pyridine‐Assisted Direct C−H/N−H Functionalization of Benzoyl Hydrazide with Isocyanide: Efficient Synthesis of Iminoisoindolinone Derivatives. Adv. Synth. Catal. 2019, 361, 16781682. DOI: 10.1002/adsc.20181801459

78. Zhang, Z.; Xie, S.; Cheng, B.; Zhai, H.*; Li, Y.* Enantioselective Total Synthesis of (+)-Arboridinine, J. Am. Chem. Soc. 2019, 141, 71477154. DOI: 10.1021/jacscaal.9b02362

77. Wang, H.; Qiu, S.; Wang, S.; Zhai, H.* Pd-Catalyzed Umpolung of p-Allylpalladium Intermediates: Assembly of All-Carbon alpha-Vinyl Quaternary Aldehydes through Csp3-Csp3 Coupling, ACS Catal. 2018, 8, 11960−11965. DOI: 10.1021/acscatal.8b03814


76. Qiu, S.; Zhai, S.; Wang, H. Tao, C.; Zhao,H.; Zhai, H.* Efficient Synthesis of Phthalimides via Cobalt-Catalyzed C(sp(2))-H Carbonylation of Benzoyl Hydrazides with Carbon Monoxide,Adv. Synth. Catal. 2018, 360, 3271−3276. DOI. 10.1002/adsc.201800388

75. Sa, S.; Liu, M.; Chen, X.; Wang, H.; Zhai, H.* Copper-catalyzed decarboxylative propargylation/hydroamination reactions: access to C3 beta-ketoester-functionalized indoles,Chem. Commun. 2018, 54, 8375−8378. DOI: 10.1039/C8CC04499F

74. Zhai, S.; Qiu,S.; Chen,X.; Tao, C.; Li, Y.; Cheng, B.; Wang, H.; Zhai, H.* Trifunctionalization of Allenes via Cobalt-Catalyzed MHP-Assisted C−H Bond Functionalization and Molecular Oxygen Activation, ACS Catal. 2018, 8, 6645−6649. DOI: 10.1021/acscatal.8b01720

73. A 2-(1-methylhydrazinyl)pyridine-directed C–H functionalization/spirocyclization cascade: facile access to spirosuccinimide derivatives,Chem. Commun. 2018, 54, 49274930. DOI: 10.1039/C8CC01774C

72. 2-(1-Methylhydrazinyl)pyridine as a reductively removable directing group in a cobalt-catalyzed C(sp2)–H bond alkenylation/annulation cascade,Chem. Commun. 2018, 54, 98101. DOI: 10.1039/C7CC08533H

71. Xiaoming Chen, Hai-Jun Zhang, Xinkan Yang, Houqiang Lv, Xiaoru Shao, Cheng Tao, Huifei Wang, Bin Cheng, Yun Li, Jingjing Guo, Jing Zhang, Zhai, H.*Divergent Total Syntheses of (-)-Daphnilongeranin B and (-)-Daphenylline, Angew. Chem. Int. Ed. 2018, 57, 947−951. DOI: 10.1002/anie.201709762

70. Duan, S.;  Cheng, B.;  Duan, X.;  Bao, B.;  Li, Y.; Zhai, H.* Synthesis of cis-5,5a,6,10b-Tetrahydroindeno 2,1-b indoles through Palladium-Catalyzed Decarboxylative Coupling of Vinyl Benzoxazinanones with Arynes. Organic Letters. 2018, 20, 1417-1420.. DOI: 10.1021/acs.orglett.8b00192

69. Li, Y.;  Yang, H.; Zhai, H.* The Expanding Utility of Rhodium-Iminocarbenes: Recent Advances in the Synthesis of Natural Products and Related Scaffolds. Chemistry-a European Journal. 2018, 24, 12757-12766. DOI: 10.1002/chem.201800689

68. Wei, J.;  Li, Y.;  Tao, C.;  Wang, H.;  Cheng, B.; Zhai, H.*; Li, Y. Organocatalytic Synthesis of 4-Aryl-1,2,3,4-tetrahydropyridines from Morita-Baylis-Hillman Carbonates through a One-Pot Three-Component Cyclization. J. Org. Chem. 2018, 83, 835-842. DOI: 10.1021/acs.joc.7b02818

67. Xu, W.;  Zhao, J.;  Tao, C.;  Wang, H.;  Li, Y.;  Cheng, B.; Zhai, H.* Collective Total Synthesis of (-)-Lundurines A-C. Organic Letters. 2018, 20, 1509-1512. DOI: 10.1021/acs.orglett.8b00210

66. Tao, Cheng; Zhang, J; Chen, X.-M; Wang, H.-F.; Li, Y; Cheng, B; Zhai, H.* Formal Synthesis of (±)-Aplykurodinone-1 through a Hetero-Pauson–Khand Cycloaddition Approach, Org. Lett. 2017, 19, 10561059. DOI: 10.1021/acs.orglett.7b00068


65. Chen, X.-Z.; Qiu S.-X.; Wang, S.-S; Wang, H.-F.; Zhai, H.* Blue-Light-Promoted Carbon-Carbon Double Bond Isomerization and Its Application in Syntheses of Quinolines, Org. Biomol. Chem. 2017, Accepted Manuscript. DOI: 10.1039/C7OB00558J


64. Chen, H.-Y.; Shao X.-R.; Wang, H.-F.; Zhai, H.* New reactivity of ethynyl benziodoxolone: modulating iron-catalyzed dehydration of propargyl alcohols, Org. Chem. Front. 2017, Advance Article DOI: 10.1039/C6QO00631K


63. Zhang, H.-J.;+ Hu, L.;+ Ma, Z.; Li, R.; Zhang, Z.; Tao, C.; Cheng, B.; Li, Y.; Wang, H.; Zhai, H.* Total Synthesis of Diterpenoid (+)-Harringtonolide, Angew. Chem. Int. Ed. 2016, 55, 1163811641. DOI: 10.1002/anie.201605879


62. Wang, S.; Chen, X.; Ao, Q.; Wang, H.;* Zhai, H.*Decarboxylative Csp3-Csp3 Coupling for Benzylation of Unstabilized Ketone Enolates: Synthesis of p-(Acylethyl)phenols, Chem. Commun.2016, 52, 94549457. DOI: 10.1039/C6CC03835B


Before 2016

61. Wei, H.; Li, Y.* Xiao, K.; Cheng, B.; Wang, H.; Hu, L.; Zhai, H.* Synthesis of Polysubstituted Pyridines via a One-Pot Metal-Free Strategy, Org. Lett. 2015, 17, 5974.

60. Zhao, H.; Yang, K.; Zheng, H.; Ding, R.; Yin, F.; Wang, N.; Li, Y.; Cheng, B.; Wang, H.; Zhai, H.* A One-Pot Synthesis of Dibenzofurans from 6-Diazo-2-Cyclohexenones, Org. Lett. 2015, 17, 5744.

59. Ding, R.; Li, Y.;* Tao, C.; Cheng, B.; Zhai, H.* Stereoselective Synthesis of (2Z)-2,4-Dienamides via NBS-Mediated Allyloxyl Addition-Claisen Rearrangement-Dehydrobromination Cascade Reaction of Ynsulfonamide, Org. Lett. 2015, 17, 3994.

58. Wang, C.; Li, Y.; Guo, R.; Tian, J.; Tao, C.; Cheng, B.; Wang, H.; Zhang, J.; Zhai, H.* Iodine-Catalyzed Facile Synthesis of Pyrolo- and Indolo[1,2-a]quinoxalines, Asian J. Org. Chem. 2015, 4, 866.

57. Chen, X.; Duan, S.; Tao, C.; Zhai, H.;* Qiu, F, G.* Total Synthesis of (+)-Gelsemine via an Organocatalytic Diels-Alder Approach, Nat. Commun. 2015, 6, 7204.

56. Guo, J.-J.; Li, Y.; Cheng, B.; Xu, T.; Tao, C.; Yang, X.; Zhang, D.; Yan, G.; Zhai, H.* Expedient Construction of the [5-6-7] Tricyclic Core of Calyciphylline A-Type Alkaloids, Asian J. Chem. 2015, 10, 865.

55. Zhao, L.; Wang, J.; Zheng, H.; Li, Y.; Yang, K.; Cheng, B.; Jin, X.; Yao, X.; Zhai, H.* Silver(I)-Catalyzed Ring-Contractive Rearrangement: A New Entry to 5-Alkylidene-2-cyclopentenones, Org. Lett. 2014, 16, 6378.

54. Ma, Z.; Cheng, B.; Zhai, H.* Synthetic Studies toward Harringtonolide, Asian J. Org. Chem. 2014, 3, 1097.

53. Tian, J.; Du, Q.; Guo, R.; Li, Y.; Cheng, B.; Zhai, H.* Total Synthesis of Indole Alkaloid (±)-Subincanadine E, Org. Lett. 2014, 16, 3173.

52. Pan, Z.; Zheng, C.; Wang, H.; Chen, Y.; Li, Y.; Cheng, B.; Zhai, H.* Total Synthesis of (±)-Sculponeatin N, Org. Lett. 2014, 16, 216–219.

51. Xu, K.; Cheng, B.; Li, Y.; Xu, T.; Yu, C.; Zhang, J.; Ma, Z.; Zhai, H.* Stereocontrolled Total Syntheses of (±)-Fawcettimine, (±)-Lycoflexine, and (±)-Lycoflexine N-Oxide, Org. Lett. 2014, 16, 196.

50. Wu, F.; Chen, Y.; Cheng, B.; Li, Y.; Zhai, H.* Synthesis of the Tetracyclic Core Structure of (±)-Nakadomarin A through Azomethine Ylide-Alkene [3+2] Cycloaddtion, Asian J. Org. Chem. 2013, 2, 561.

49. Wu, F.; Dong, M.; Fang, F.; Sang, Y.; Li, Y.; Cheng, B.; Zhang, L.;* Zhai, H.* Direct Access to Tetrahydro[1,2]diazepinones from a,b-Epoxy-N-Aziridinylimines via Anionic Rearrangement, Org. Lett. 2013, 15(4), 914.

48. Yang, K.; Zhang, J.; Li, Y.; Cheng, B.; Zhao, L.; Zhai, H.* Facile Synthesis of 2-Arylphenols via Palladium-Catalyzed Cross-Coupling of Aryl Iodides with 6-Diazo-2-cyclohexenones, Org. Lett. 2013, 15(4), 808.

47. Yang, Y.; Fu, X.; Chen, J.; Zhai, H.* Total Synthesis of (–)-Jiadifenin, Angew. Chem. Int. Ed. 2012, 51, 9825.

46. Chen, J.; Gao, P.; Yu, F.; Yang, Y.; Zhu, S.; Zhai, H.* Total Synthesis of (±)-Merrilactone A, Angew. Chem. Int. Ed. 2012, 51, 5897.

45. Xie, Y.; Wang, N.; Cheng, B.; Zhai, H.* Total Synthesis of (±)-Cephalosol, Org. Lett. 2012, 14, 3.

44. Song, Z.; Zhao, Y.-M.;* Zhai, H.* One-Step Construction of Tetrahydro-5H-indolo[3,2-c]quinolines from Benzyl Azides and Indoles via a Cascade Reaction Sequence, Org. Lett. 2011, 13, 6331.

43. Yu, F.; Cheng, B.; Zhai, H.* Fast and Protecting-Group-Free Synthesis of (±)-Subincanadine C, Org. Lett. 2011, 13, 5782-5783.

42. Cheng, B.; Wu, F.; Yang, X.; Zhou, Y.; Wan, X.; Zhai, H.* Efficient Total Synthesis of Marine Alkaloid (–)-Nakadomarin A, Chem.Eur. J. 2011, 17, 12569-12572.

41. Yu, F.; Li, G.; Gao, P.; Gong, H.; Liu, Y.; Wu, Y.; Cheng, B.; Zhai, H.* Concise Synthesis of the Oxapentacyclic Core of Cortistatin A, Org. Lett. 2010, 12, 5135.

40. Zhang, W.; Yang, X.; Chen, W.; Xu, X.; Li, L.; Zhai, H.*; Li, Z.* Design, Multicomponent Synthesis, and Bioactivities of Novel Neonicotinoid Analogues with 1,4-Dihydropyridine Scaffold, J. Agric. Food Chem. 2010, 58, 2741.

39. Gong, H.; Jia, X.;* Zhai, H.* New Progress of the Application of Samarium Diiodide in Organic Synthesis, Chin. J. Org. Chem. 2010, 30, 939.

38. Xu, Q.; Cheng, B.; Ye, X.;* Zhai, H.* SmI2–Mediated Carbon–Carbon Bond Fragmentation in α-Aminomethyl Malonates, Org. Lett. 2009, 11, 4136.

37. Hu, L.; Zhang, L.;* Zhai, H.* Syntheses and Configuration Determination of (+)-Villatamines A and B, Two Marine Natural Products, J. Org. Chem. 2009, 74, 7552.

36. Li, G.; Yang, X.; Zhai, H.* Total Synthesis of (–)-5,6-Dihydrocineromycin B, J. Org. Chem. 2009, 74, 1356.

35. Gao, P.; Xu, P.-F.; Zhai, H.* Expeditious Construction of (+)-Mintlactone via Intramolecular Hetero-Pauson-Khand Reaction, J. Org. Chem. 2009, 74, 2592.

34. Wei, H.; Zhai, H.; Xu, P.-F.* Novel Platinum-Catalyzed Tandem Reation: An Efficient Approach to Construct Naphtho[1,2-b]furan, J. Org. Chem. 2009, 74, 2224.

33. Cheng, B.; Zhai, H.* Studies on Fluorinated Annulated Nicotines. Concise Synthesis of cis-4,4-difluoro-2,3,3a,4,5,9b-Hexahydro-l-methy1-lH-pyrrolo[2,3-f]quinoline, Synlett 2009, 1955.

32. Gao, P.; Tong, Z.; Hu, H.; Xu, P.-F.; Liu, W.; Sun, C.; Zhai, H.* Synthesis of (+)-9a-epi-Stemoamide via DBU-Catalyzed Michael Addition of Nitroalkane, Synlett 2009, 2188.

31. Deng, H.; Yang, X.; Tong, Z.; Li, Z.; Zhai, H.* Expedient Synthesis of the Tetracyclic Core of ent-Nakadomarin A, Org. Lett. 2008, 10, 1791.

30. Yang, X.; Zhai, H.;* Li, Z.* Enantiocontrolled Synthesis of (–)-9-epi-Pentazocine and (–)-Aphanorphine, Org. Lett. 2008, 10, 2457.

29. Sang, Y.; Zhao, J.; Jia, X.; Zhai, H.* Asymmetric Synthesis of (+)-Pyrido[3,4-b]homotropane, J. Org. Chem. 2008, 73, 3589.

28. Yang, X.; Cheng, B.; Li, Z.*; Zhai, H.* Formal Asymmetric Synthesis of (–)-Aphanorphine via RCM Reaction, Synlett 2008, 2821.

27. Tong, Z.; Gao, P.; Deng, H.; Xu, P.-F.; Zhai, H.* Propylene Oxide-Assisted Sonogashira Coupling Reaction, Synlett 2008, 3239.

26. Yang, X.; Zhu, L.; Zhou, Y.; Li, Z.;* Zhai, H.* Efficient Synthesis of Monosubstituted 3-Alkynylfurans via Suzuki Coupling, Synthesis 2008, 1729.

25. Zhou, Y.; Xu, Q.; Zhai, H.* A Stereocontrolled Approach to (±)-Nonactic Acid, Tetrahedron Lett. 2008, 49, 5271.

24. Gao, P.; Xu, P.-F.; Zhai, H.* Borax-Catalyzed Thiolysis of 1,2-Epoxides in Aqueous Medium, Tetrahedron Lett. 2008, 49, 6536.

23. Ma, Z.; Zhai, H.* A Concise Formal Synthesis of Unnatural (+)-Aphanorphine from (2S,4R)-4-Hydroxyproline, Synlett 2007, 161.

22. Ma, Z.; Hu, H.; Xiong, W; Zhai, H.* Formal Syntheses of (–) and (+)-Aphanorphine from (2S,4R)-4-Hydroxyproline, Tetrahedron 2007, 63, 7523.

21. Kong, L.; Zhuang, Z.; Chen, Q.; Deng, H.; Tang, Z.; Jia, X.; Li, Y.; Zhai, H.* A Facile Asymmetric Synthesis of (+)-Eldanolide, Tetrahedron: Asym. 2007, 18, 451.

20. Liu, Y.; Luo, S.; Fu, X.; Fang, F.; Zhuang, Z.; Xiong, W.; Jia, X.; Zhai, H.* Facile Construction of the Pentacyclic Framework of Subincanadine B. Synthesis of 20-Deethylenylated Subincanadine B and 19,20-Dihydrosubincanadine B, Org. Lett. 2006, 8, 115.

19. Gao, P.; Liu, Y.; Zhang, L.; Xu, P.-F.; Wang, S.; Lu, Y.; He, M.; Zhai, H.* Total Synthesis of Indole Alkaloid (±)-Subincanadine F via SmI2-Mediated Ring-Opening and Bridge-Forming Mannich Reaction, J. Org. Chem. 2006, 71, 9495.

18. Yang, X.; Luo, S.; Fang, F.; Liu, P.; Lu, Y.; He, M.; Zhai, H.* Synthesis of conformationally restricted nicotine analogues by intramolecular [3 + 2] cycloaddition, Tetrahedron 2006, 62, 2240.

17. Zhuang, Z.; Zhang, W.; Jia, X.;* Zhai, H. Application of Titanocene Monochloride to Organic Synthesis, Chin. J. Org. Chem. 2006, 26, 145.

16. Zhang, W.; Luo, S.; Fang, F.; Chen, Q.; Hu, H.; Jia, X.; Zhai, H.* Total Synthesis of Absinthin, J. Am. Chem. Soc. 2005, 127, 18–19.

15. Ye, W.; Cai, G.; Zhuang, Z.; Jia,X.; Zhai, H.* One-Step Assembly of Functionalized γ-Butyrolactones from Benzoins or Benzaldehydes via an N-Heterocyclic Carbene-Mediated Tandem Reaction, Org. Lett. 2005, 7, 3769.

14. Chen, Q.; Deng, H.; Zhao, J.; Lu, Y.; He, M.; Zhai, H.* Two efficient four-step routes to marine toxin tanikolide, Tetrahedron 2005, 61, 8390.

13. Luo, S.; Zhao, J.; Zhai, H.* A Fast Assembly of Pentacyclic Benz[f]indolo[2,3-a]quinolizidine Core by Tandem Intermolecular Formal Aza-[3 + 3] Cycloaddition/Pictet-Spengler Cyclization: A Formal Synthesis of (±)-Tangutorine, J. Org. Chem. 2004, 69, 4548.

12. Luo, S; Fang, F.; Zhao, M.; Zhai, H.* A One-Pot Assembly of 4-Allyl-3-pyridinecarboxaldehyde. A New Synthesis of 1-Methyl-1,2,3,3a,4,8b-hexahydropyrrolo[3,2-f]pyrindine, an Annulated Nicotine Analogue, Tetrahedron 2004, 60, 5353.

11. Yang, X.; Hua, C.*; Zhai, H.* Synthesis of Monoterpene Pyridine Alkaloid Aucubinine A, Chin. J. Org. Chem. 2004, 24, 1429.

10. Zhai, H.*; Luo, S.; Ye. C.; Ma, Y. A Facile Asymmetric Route to (–)-Aphanorphine, J. Org. Chem. 2003, 68, 8268.

9. Hu, H.; Zhai, H.* An Efficient Synthesis of (1R,4S)-1-Methyl-8-methoxy-3-(4-toluenesulfonyl)-2,3,4,5-tetrahydro-1,4-methano-3-benzazepine. A Formal Synthesis of (–)-Aphanorphine, Synlett 2003, 2129.

8. Zhao, J.; Yang, X.; Jia, X.; Luo, S.; Zhai, H.* Novel Total Syntheses of (±)-Oxerine Using an Intramolecular Heck Reaction as a Key Step, Tetrahedron 2003, 59, 9379.

7.Yang, X.; Luo, S.; Hua, C.; Zhai, H.* Efficient Synthesis of Beetle Aggregation Pheromone Frontalin and Its Analogues, Tetrahedron 2003, 59, 8551.

6. Zhai, H.*; Chen, Q.; Zhao, J.; Luo, S.; Jia, X. A New Synthesis of Tanikolide, Tetrahedron Lett. 2003, 44, 2893.

5. Zhao, J.; Jia, X.; Zhai, H.* A New Mild Regioselective Bromination of Arylamines, Tetrahedron Lett. 2003, 44, 9371.

4. Yang, X.; Zhao, J.; Jia, X.; Yang, L.; Zhai, H.* A Concise Synthesis of Monoterpene Pyridine Alkaloid Aucubinine B, Chin. J. Chem. 200321, 970.

3. Zhai, H.*; Liu, Z.-Y.* The Highlights of the Organic Chemistry in 2002, Chin. J. Org. Chem. 2003, 23, 885.

2. Zhao, J.; Jia, X.*; Zhai, H. Application of SmI2 in Organic Synthesis, Chin. J. Org. Chem. 2003, 23, 499.

1. Zhai, H.*; Liu, P.; Luo, S.; Fang, F.; Zhao, M. A Facile Synthesis of cis-1-Methyl-1,2,3,3a,4,8b-hexahydropyrrolo[3,2-f]pyrindine, an Annulated Nicotine Analog, Org. Lett. 2002, 4, 4385.