Publications


79. (Account) Adventures in Total Synthesis – The Next Chapter. (Dedicated to Professor Ian Paterson and Professor K. C. Nicolaou) Synlett. 2024, 35, 1345-1360 (Invited contribution to Synlett Account by Peter C. Vollhardt)

78. Stereo-controlled Synthesis of Vicinal Tertiary Carbinols: Application in the Synthesis of a Diol Substructure of Zaragozic Acid, Pactamycin and Ryanodol. Chem. Eur. J. 2023, 29, e202301938 (Dedicated to Professor Ian Paterson on the occasion of his retirement)

77. (Book Chapter) Contemporary Accounts in Drug Discovery and Development: Chapter 15 Accelerating Drug Discovery and Development: Translational Medicine in Combating the COVID-19 Pandemic (With X. Huang and W. H. Tang, Pages: 385-420). Ed. X. Huang, R. G. Aslanian, and W. H. Tang, John Wiley & Sons, Inc. 2022


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76. (Book Chapter) Contemporary Accounts in Drug Discovery and Development: Chapter 14 Combination Therapy Case Studies in Anticancer and Anti-Infectious Disease Drug Discovery and Development (With X. Huang, Pages: 341-384). Ed. X. Huang, R. G. Aslanian, and W. H. Tang, John Wiley & Sons, Inc. 2022


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75. Late-Stage and Strain-Accelerated Oxidation Enabled Synthesis of Haouamine A. Chem. Sci., 2020, 11, 8132-8137

74. (Author Profile) Angew. Chem. Int .Ed. 2019, 58, 13624

73. A Local-Desymmetrization-Based Divergent Synthesis of Quinine and Quinidine. Angew. Chem. Int. Ed. 2019, 58, 488-493 (In memory of Professor Gilbert Stork)

72. A Desymmetrization-Based Total Synthesis of Reserpine. Angew. Chem. Int. Ed. 2018, 57, 16152-16156 (Cover page) (Dedicated to Professor E. J. Corey on the occasion of his 90th birthday)

71. (Essay) A Personal Perspective on Organic Synthesis: Past, Present, and Future, Special Issue: Rosarium Philosophorum - Organic Synthesis. Isr. J. Chem. 2018, 58, 85-93 (Dedicated to Professor Dieter Seebach on the occasion of his 80th birthday)

70. A Desymmetrization-Based Approach to Morphinans: Application in the Total Synthesis of Oxycodone. Chem. Commun., 2018, 54, 13018-13021

69. Total Synthesis of Strychnine. Chem. Eur. J. 2017, 23, 16189-16193 (Dedicated to Professor Robert Burns Woodward)

68. Asymmetric Total Syntheses of Communesin F and a Putative Member of the Communesin Family. Angew. Chem. Int. Ed. 2017, 56, 14237-14240 (In memory of Carlos F. Barbas III)

67. Organocatalytic and Late-Stage CH-Functionalization Enabled Asymmetric Synthesis of Communesin F and Putative Communesins (Special Issue: Synthesis of Antibiotics and Related Molecules). J. Org. Chem. 2018, 83, 6936-6957

66. An Asymmetric Pathway to Dendrobine by a Transition-Metal-Catalyzed Cascade Process. Angew. Chem. Int. Ed. 2017, 56, 12250-12254

65. Total Synthesis of Actinophyllic Acid. Angew. Chem. Int. Ed. 2017, 56, 12277-12281 (Dedicated to Professor Yoshito Kishi on the occasion of his 80th birthday)

64. Programmed Serial Stereochemical Relay and its Application in the Synthesis of Morphinans. Chem. Sci., 2017, 8, 7031

63. (Highlights) Synthesis of the C18-Norditerpenoid Alkaloid Neofinaconitine: A Lesson in Convergent Synthesis Planning. Angew. Chem. Int. Ed. 2014, 53, 924-926 (In memory of David Y. Gin)

62. (Editorial) Transition-metal and organocatalysis in natural product synthesis (with D. Ma) Beilstein J. Org. Chem. 2013, 9, 1192-1193

61. (Book Chapter) Modern Tools for the Synthesis of Complex Bioactive Molecules: Metathesis-based Synthesis of Complex Bioactives. Ed. J. Cossy and S. Arseniyandis, John Wiley & Sons, Inc. 2012

60. (Review) A Case Study of Single-Pill Combination Therapy: The Ezetimibe/Simvastatin Combination for Treatment of Hyperlipidaemia (with X. Huang) ChemMedChem. 2012, 7, 1882-1894

59. (Review) Recent Advances in the Total Synthesis of Cyclopropane Containing Natural Products. Chem. Soc. Rev. 2012, 41, 4631-4642

58. (Review) C–H Activation: A Complementary Tool in the Total Synthesis of Complex Natural Products. (with S. W. Youn) Chem. Eur. J. 2012, 18, 9452-9474 (Dedicated to Professor Gilbert Stork on the occasion of his 90th birthday)

57. A Mast Cell Degranulation Screening Assay for the Identification of Novel Mast Cell Activating Agents. MedChemComm. 2013, 4, 88-94 (New Talent Issue, Invited by Co-Editor-in-Chief: Gregory Verdine)

56. (Review) The Chemistry of the Polycyclic Polyprenylated Acylphloroglucinols (PPAPs) Angew. Chem. Int. Ed. 2012, 51, 4536-4561 (In memory of David Y. Gin)

55. A Chiral-Pool Based Approach to the Core Structure of (+)-Hyperforin. Eur. J. Org. Chem. 2012, 3, 484-487

54. (Review) Chemical Synthesis of the Englerins (Dedicated to Professor K. C. Nicolaou for his contribution in chemical education in Singapore and on the occasion of his 65th birthday) Chem. Asian J. 2012, 7, 22-35 (Invited contribution by Editor-in-Chief: Peter Gölitz)

53. (Account) Adventures in Total Synthesis – A Personal Account. (Dedicated to Professor K. C. Nicolaou on the occasion of his 65th birthday) Synlett. 2011, 17, 2459-2481 (Invited contribution to Synlett Account by Editor-in-Chief: Peter C. Vollhardt)

52. Lagunamide C, a Cytotoxic Cyclodepsipeptide from the Marine Cyanobacterium Lyngbya majuscule. Phytochemistry 2011, 18, 2369-2375

51. Total Synthesis of Echinopines A and B: Exploiting a Bioinspired Late-Stage Intramolecular Cyclopropanation. Org. Lett. 2011, 13, 5724–5727

50. A Modular Synthesis of Salvileucalin B Structural Domains. Org. Lett. 2011, 13, 4410-4413


From Institute of Chemical and Engineering Sciences, A*STAR (SINGAPORE):


49. Synthesis of ent-Nanolobatolide. Angew. Chem. Int. Ed. 2011, 50, 4165-4168

48. Synthesis of an Advanced Maoecrystal V Core Structure. Chem. Eur. J. 2011, 17, 5778-5781

47. Proteomic Signature of Fatty Acid Biosynthesis Inhibition Available for In-Vivo Mechanism-of-Action Studies. Antimicrob. Agents Chemother. 2011, 55, 2590-2596

46. Formal Asymmetric Synthesis of Echinopine A and B. Angew. Chem. Int. Ed. 2011, 50, 3013-3016

45. Chemical Synthesis and Biological Evaluation of the Englerin Analogues. ChemMedChem. 2011, 6, 420-423

44. A Second-Generation Formal Synthesis of (+)-Haplophytine. Eur. J. Org. Chem. 2011, 1027-1031

43. Formal Syntheses of (-)- and (+)-Phalarine. Angew. Chem. Int. Ed. 2011, 50, 676-679

42. Chemical Synthesis and Biological Evaluation of Second-Generation Palmerolide A Analogues. Eur. J. Org. Chem. 2011, 463-468

41. Total Synthesis and Biological Evaluation of Fab-Inhibitory Antibiotic Platencin and Analogues Thereof. Eur. J. Org. Chem. 2011, 183-196

40. (Review) Chemistry of the Cortistatins – A Novel Class of Anti-Angiogenic Agents. Org. Biomol. Chem. 2010, 8, 2900-2911 (Invited Perspective)

39. Modular Synthesis of Polyphenolic Benzopyrans, and Application in the Total Synthesis of Malibatol A and Shoreaphenol. Molecules 2010, 15, 5909-5927 (Invited contribution to special issue: Diversity Oriented Synthesis, Guest Editor: Peter Wipf)

38. Total Synthesis of Englerin A. J. Am. Chem. Soc. 2010, 132, 8219-8222

37. Total Synthesis and Biological Evaluation of the Resveratrol-Derived Polyphenol Natural Products Hopeanol and Hopeahainol A. J. Am. Chem. Soc. 2010, 132, 7540-7548

36. Total Synthesis of Echinopines A and B. J. Am. Chem. Soc. 2010, 132, 3815-3818

35. Synthesis of Functionalized Maoecrystal V Core Structures. Chem. Comm. 2010, 46, 70-72

34. Total Synthesis of (+)-Haplophytine. Angew. Chem. Int. Ed. 2009, 48, 7616-7620

33. Cortistatin A is a High-Affinity Ligand of Protein Kinases ROCK, CDK8, and CDK11. Angew. Chem. Int. Ed. 2009, 48, 8952-8957

32. Identification of Distinct Thiopeptide-Antibiotic Precursor Lead Compounds Using Translation Machinery Assays. Chem. Biol. 2009, 16, 1087-1096

31. Total Synthesis and Biological Evaluation of Cortistatin A and J and Analogues Thereof. J. Am. Chem. Soc. 2009, 131, 10587-10597

30. Total Synthesis of Hopeahainol A and Hopeanol. Angew. Chem. Int. Ed. 2009, 48, 3440-3443

29. New Synthetic Technologies for the Construction of Heterocycles and Tryptamines. J. Am. Chem. Soc. 2009, 131, 3690-3699

28. Total Synthesis of (+)-Cortistatin A. Angew. Chem. Int. Ed. 2008, 47, 7310-7313

27. An Expedient Asymmetric Synthesis of Platencin. J. Am. Chem. Soc. 2008, 130, 11292-11293

26. Chemical Synthesis and Biological Evaluation of Palmerolide A Analogues. J. Am. Chem. Soc. 2008, 130, 10019-10023

25. Total Synthesis of Amythiamicins A, B and C. Chem. Comm. 2008, 12, 2632-2634

24. An Expedient Strategy for the Synthesis of Tryptamines and Other Heterocycles. Angew. Chem. Int. Ed. 2008, 47, 4217-4220

23. Total Synthesis of the Originally Proposed and Revised Structures of Palmerolide A and Isomers Thereof. J. Am. Chem. Soc. 2008, 130, 3633-3644

22. Total Syntheses of Thiopeptide Antibiotics GE2270A, GE2270T, and GE2270C1. Chem. Asian J. 2008, 3, 413-429

21. A Chiral Pool Based Synthesis of Platensimycin. Angew. Chem. Int. Ed. 2008, 47, 944-946

20. Total Synthesis of the Originally Proposed and Revised Structures of Palmerolide A. Angew. Chem. Int. Ed. 2007, 46, 5896-5900

19. Construction of the “Left Domain” of Haplophytine. Angew. Chem. Int. Ed. 2007, 46, 4715-4718

18. Total synthesis of antibiotics GE2270A and GE2270T. Angew. Chem. Int. Ed. 2006, 45, 7786-7792


From University of Cambridge (Ph.D., with Professor Ian Paterson) and

The Scripps Research Institute (Postdoc, with Professor K. C. Nicolaou):


17. Total Synthesis and Structural Elucidation of Azaspiracid-1. Final Assignment and Total Synthesis of the Correct Structure of Azaspiracid-1. Nicolaou K. C.,* Koftis T. V., Vyskocil S., Petrovic G., Tang W., Frederick M. O., Chen D. Y.-K., Li Y., Ling T., Yamada Y. M. A. J. Am. Chem. Soc. 2006, 128, 2859-2872

16. Total Synthesis and Structural Elucidation of Azaspiracid-1. Synthesis-Based Analysis of Originally Proposed Structures and Indication of Their Non-Identity to the Natural Product. Nicolaou K. C.,* Chen D. Y.-K., Li Y., Uesaka N., Petrovic G., Koftis T. V., Bernal F., Frederick M. O., Govindasamy M., Ling T., Pihko P. M., Tang W., Vyskocil S. J. Am. Chem. Soc. 2006, 128, 2258-2267

15. Total Synthesis of Altohyrtin A/Spongistatin 1. Part 4: Fragment Couplings, Completion of the Synthesis, Analogue Generation and Biological Evaluation. Paterson I.,* Chen D. Y.-K., Coster M. J., Aceña J. L., Bach J., Wallace D. J. Org. Biomol. Chem. 2005, 3, 2431-2440

14. Total Synthesis of Altohyrtin A/Spongistatin 1. Part 3: The Southern Hemisphere EF Segment. Paterson I.,* Coster M. J., Chen D. Y.-K., Aceña J. L., Bach J., Keown L. E., Trieselmann T. Org. Biomol. Chem. 2005, 3, 2420-2430

13. The Stereocontrolled Total Synthesis of Altohyrtin A/Spongistatin 1. Part 2: The CD-Spiroacetal Segment. Paterson I.,* Coster M. J., Chen D. Y.-K., Gibson K. R., Wallace D. J. Org. Biomol. Chem. 2005, 3, 2410-2419

12. The Stereocontrolled Total Synthesis of Altohyrtin A/Spongistatin 1. Part 1: The AB-Spiroacetal Segment. Paterson I.,* Coster M. J., Chen D. Y.-K., Oballa R. M., Wallace D. J., Norcross R. D. Org. Biomol. Chem. 2005, 3, 2399-2409

11. Chemistry and Biology of Diazonamide A: Second Total Synthesis and Biological Investigations. Nicolaou K. C.,* Hao J., Reddy M. V., Rao P. B., Rassias G., Snyder S. A., Huang X., Chen D. Y.-K., Brenzovich W. E., Giuseppone N., Giannakakou P., O’Brate A. J. Am. Chem. Soc. 2004, 126, 12897-12906

10. Chemistry and Biology of Diazonamide A: First Total Synthesis and Confirmation of the True Structure. Nicolaou K. C.,* Chen D. Y.-K., Huang X., Ling T., Bella M., Snyder S. A. J. Am. Chem. Soc. 2004, 126, 12888-12896

9. Structural Revision and Total Synthesis of Azaspiracid-1, Part 1: Intelligence Gathering and Tentative Proposal. Nicolaou K. C.,* Vyskocil S., Koftis T. V., Yamada Y. M. A., Ling T., Chen D. Y.-K., Tang W., Petrovic G., Frederick M. O., Li Y., Satake M. Angew. Chem. Int. Ed. 2004, 43, 4312-4318

8. Total Synthesis of the Proposed Azaspiracid-1 Structure, Part 2: Coupling of the C1-C20, C21-C27, and C28-C40 Fragments and Completion of the Synthesis. Nicolaou K. C.,* Chen D. Y.-K., Li Y., Qian W., Ling T., Vyskocil S., Koftis T. V., Govindasamy M., Uesaka N. Angew. Chem. Int. Ed. 2003, 42, 3649-3653

7. Total Synthesis of the Proposed Azaspiracid-1 Structure, Part 1: Construction of the Enantiomerically Pure C1-C20, C21-C27, and C28-C40 Fragments. Nicolaou K. C.,* Li Y., Uesaka N., Koftis T. V., Vyskocil S., Ling T., Govindasamy M., Qian W., Bernal F., Chen D. Y.-K. Angew. Chem. Int. Ed. 2003, 42, 3643-3648

6. The Second Total Synthesis of Diazonamide A. Nicolaou K.C.,* Rao P. B., Hao J., Reddy M. V., Rassias G., Huang X., Chen D. Y.-K., Snyder S. A. Angew. Chem. Int. Ed. 2003, 42, 1753-1758

5. Synthesis and Biological Evaluation of Spongistatin/Altohyrtin analogues: E-ring Dehydration and C46 Side-chain Truncation. Paterson I.,* Aceña J. L., Bach J., Chen D. Y.-K., Coster M. J. Chem. Comm. 2003, 4, 462-463

4. Total Synthesis of Diazonamide A. Nicolaou K.C.,* Bella M., Chen D. Y.-K., Huang X., Ling T., Snyder S.A. Angew. Chem. Int. Ed. 2002, 41, 3495-3499

3. Total Synthesis of Siphonarin B and Dihydrosiphonarin B. Paterson I.,* Chen D. Y.-K., Franklin A. S. Org. Lett. 2002, 4, 391-394

2. Stereocontrolled Total Synthesis of (+)-Altohyrtin A/Spongistatin 1. Paterson I.,* Chen D. Y.-K., Coster M. J., Aceña J. L., Bach J., Gibson K. R., Keown L. E., Oballa R. M., Trieselmann T., Wallace D. J., Hodgson A., Norcross R. D. Angew. Chem. Int. Ed. 2001, 40, 4055-4060

1. Studies in Marine Polypropionate Synthesis: Total Synthesis of (-)-Baconipyrone C. Paterson I.,* Chen D. Y.-K., Aceña J. L., Franklin A. S. Org. Lett.2000, 2, 1513-1516