Publications

Type of Publication:
69 : "Dearomatization Approach to 2-Trifluoromethylated Benzofuran and Dihydrobenzofuran Products" Smith, D. T.; Vitaku, E.; Njardarson J. T. Org. Lett. 2017, 19, ASAP

Type of Publication: Publication
68 : "A Mild Meta-Selective C-H Alkylation of Catechol Mono-Ethers" Vitaku, E.; Njardarson, J. T. Eur. J. Org. Chem. 2016, 3679.

67 : "Anionic Cascade Routes to Sulfur and Nitrogen Heterocycles Originating from Thio- and Aminophosphate Precursors" Das, P.; Njardarson, J. T. Eur. J. Org. Chem. 2016, 4249.

66 : "Metal-Free Synthesis of Fluorinated Indoles Enabled by Oxidative Dearomatization" Vitaku, E.; Smith, D. T. ; Njardarson, J. T. Angew. Chem. Int. Ed. 2016, 55, 2243.

65 : "Asymmetric [3+2] Annulation Approach to 3-Pyrrolines:  Concise Total Syntheses of (-)-Supinidine, (-)-Isoretronecanol and (+)-Elacomine" Chogii, I.; Njardarson, J. T. Angew. Chem. Int. Ed. 2015, 54, 13706.

64 : “Synthesis of 1,2,3,6-Tetrahydropyridines via Aminophosphate Enabled Anionic Cascade and Acid Catalyzed Cyclization Approaches” Das, P.; Njardarson, J. T. Org. Lett. 2015, 17, 4030.

63 : "Synthetic Approaches and Total Syntheses of Vinigrol, a Unique Diterpenoid" Draghici, C.; Njardarson, J. T. Tetrahedron 2015, 71, 3775.

62 : "Ring Expansions of Oxiranes and Oxetanes" Smith, D. T.; Njardarson, J. T. Topics in Heterocyclic Chemistry 2015, 41, 281.
61 : "Formation of Fused Aromatic Architectures via an Oxidative Dearomatization - Radical Cyclization Rearomatization Approach" Vitaku, E.; Njardarson, J. T. Tetrahedron Lett. 2015, 56, 3550 (Special issue in honor of Professor H. H. Wasserman)

60 : “The Realization of an Oxidative Dearomatization-Intramolecular Diels-Alder Route to Vinigrol”, Draghici, C.; Njardarson, J. T. Strategies and Tactics in Organic Synthesis 11 (Book chapter) 2015, accepted.
59 : "Beyond C, H, O and N!  Analysis of the Elemental Composition of US FDA Approved Drug Architectures" Smith, B. R.; Eastman, C. M.; Njardarson, J. T. J. Med. Chem. 2014, 57, 9764.

58 : "Analysis of the Structural Diversity, Substitution Patterns and Frequency of Nitrogen Heterocycles among US FDA Approved Pharmaceuticals" Vitaku, E.; Smith, D. T.; Njardarson, J. T. J. Med. Chem. 2014, 57, 10257.

57 : "Mild Stereoselective Formation of Tri- and Tetrasubstituted Olefins by Regioselective Ring Opening of 1,1-Disubstituted Vinyl Oxiranes with Dialkyl Dithiophosphates" Guo, B.; Vitaku, E.; Njardarson, J. T. Tetrahedron Lett. 2014, 55, 3232.

56 : "A Scalable Rhodium-Catalyzed Intermolecular Aziridination Reaction" Smith, D. T.; Njardarson, J. T. Angew. Chem. Int. Ed. 2014, 53, 4278.
55 : "Evolution of an Oxidative Dearomatization Enabled Total Synthesis of Vinigrol" Yang, Q.; Draghici, C.; Njardarson, J. T.; Li, F.; Smith, B. R.; Das, P. Org. Biomol. Chem. 2014, 12, 330.                                        (Selected as an OBC Hot article)

54 : "Base Mediated Deprotection Strategies for Trifluoroethyl (TFE) Ethers, a New Alcohol Protecting Group" Yang, Q.; Njardarson, J. T. Tetrahedron Lett. 2013, 54, 7080.

53 : "Data-mining for Sulfur and Fluorine:  An Evaluation of Pharmaceuticals To Reveal Opportunities for Drug Design and Discovery" Ilardi, E. A.; Vitaku, E.; Njardarson, J. T. J. Med. Chem. 2014, 57, 2832.

52 : “Z-Selective Ring Opening of Vinyl Oxetanes with Dialkyl Dithiophosphate Nucleophiles” Guo, B.; Njardarson, J. T. Chem. Commun. 2013, 49, 10802.

51 : “Ring Expansions of Vinyl- Oxiranes, Thiiranes and Aziridines: Synthetic Approaches, Challenges and Catalytic Success Stories” Ilardi, E. A.; Njardarson, J. T.  J. Org. Chem. 2013, 78, 9533.

50 : "An In-Pharm-ative Educational Poster Anthology Highlighting the Therapeutic Agents that Chronicle Our Medicinal History" Ilardi, E. A.; Vitaku, E.; Njardarson, J. T. J. Chem. Ed. 2013, 90, 1403.

49 : "Total Synthesis of Vinigrol" Yang, Q.; Njardarson, J. T.; Draghici, C.; Li, F. Angew. Chem. Int. Ed. 2013, 52, 8648.     (Featured April 7th 2014 By Professor Taber on Organic Chemistry Portal)          Vinigrol featured in the October 2013 issue of Synform

48 : "Catalytic Ring Expansion Adventures" Njardarson, J. T. Synlett, 2013, 787 (Invited Account)

47 : "Recent Advances in the Metal-Catalyzed Ring Expansions of Three- and Four-Membered Rings" Mack, D. J.; Njardarson, J. T. ACS Catal. 2013, 3, 272.

46 : "Mechanism and the Origins of Stereospecificity in Copper Catalyzed Ring Expansion of Vinyl Oxiranes: A Traceless Dual Transition Metal-Mediated Process" Mustard, T. J. L.; Mack, D. J.; Njardarson, J. T.; Cheong, Paul. H.-Y. J. Am. Chem. Soc. 2013, 135, 1471.

45 : "Syntheses and Structural Confirmations of Members of a Heterocycle-Containing Family of Labdane Diterpenoids" Mack, D. J.; Njardarson, J. T. Angew. Chem. Int. Ed. 2013, 52, 1543.

44 : "New Mechanistic Insights into the Copper Catalyzed Ring Expansion of Vinyl Aziridines:  Evidence in Support of a Copper(I) Mediated Pathway" Mack, D. J.; Njardarson, J. T. Chem. Sci. 2012, 3, 3321.

43 : "Reactions at your fingertips" Njardarson, J. T. Nature Chem. 2012, 4, 590.
42 : "Distinct Biological Effects of Golgicide A Derivatives on Larval and Adult Mosquitos" Mack, D. J.; Isoe, J.; Miesfeld, R. L.; Njardarson, J. T. Bioorg. Med. Chem. Lett. 2012, 22, 5177.

41 : "Synthesis of Allylic and Homoallylic Alcohols from Unsaturated Cyclic Ethers Using a Mild and Selective C-O Reduction Approach" Mack, D. J.; Guo, B.; Njardarson J. T. Chem. Commun. 2012, 48, 7844.

40 : "Catalytic Ring Expansion of VInyl Oxetanes:  Asymmetric Synthesis of Dihydropyrans Using Chiral Counterion Catalysis" Guo, B.; Schwarzwalder, G.; Njardarson, J. T. Angew. Chem. Int. Ed. 2012, 51, 5675.

39 : "Chemistry By Design - A Web Based Educational Flashcard for Exploring Synthetic Organic Chemistry" Draghici, C.; Njardarson, J. T. J. Chem. Ed. 2012, 89, 1080.

38 : "Pharmaceutical Structure Montages as Catalysts for Design and Discovery" Njardarson, J. T. Future Med. Chem. 2012, 4, 951.
37 : "Efficient Synthesis of Thiopyrans Using Sulfur-Enabled Anionic Cascade" Li, F.; Calabrese, D.; Brichacek, M.; Lin, I.; Njardarson, J. T. Angew. Chem. Int. Ed. 2012, 51, 1938.

36 : "Intermolecular Oxonium Ylide Mediated Synthesis of Medium-Sized Ocacycles" Mack, D. J.; Batory, L. A.; Njardarson, J. T. Org. Lett. 2012, 14, 378.

35 : "Emergence of Potent Inhibitors of Metastasis in Lung Cancer vis Syntheses Based on Migrastatin" Lecomte, N.; Njardarson, J. T.; Nagorny, P.; Yang, G.; Downey, R.; Ouerfelli, O.; Moore, M. A. S.; Danishefsky, S. J. Proc. Natl. Acad. Sci. U. S. A. 2011, 108, 15074.
34 : “Synthetic Efforts Toward [3.3.1] Bridged Bicyclic Phloroglucinol Natural Products” Njardarson, J. T. Tetrahedron 2011, 67, 7631 (Invited Report).

33 : “Stereospecific Ring Expansion of Chiral Vinyl Aziridines” Brichacek, M.; Navarro Villalobos, M.; Plichta, A.; Njardarson J. T. Org. Lett. 2011, 13, 1110.

32 : “An Efficient Oxidative Dearomatization-Radical Cyclization Approach to Symmetrically Substituted Bicyclic Guttiferone Natural Products” McGrath, N. A.; Binner, J. R.; Markopoulos, G.; Brichacek, M.; Njardarson J. T. Chem. Commun. 2011, 47, 209.

31 : “The Strategic Marriage of Method and Motif. Total Synthesis of Varitriol” Brichacek, M.; Batory, L. A.; McGrath, N. A.; Njardarson J. T. Tetrahedron 2010, 66, 4832.

30 : “A Graphical Journey of Innovative Organic Architectures That Have Improved Our Lives” McGrath, N. A.; Brichacek, M.; Njardarson J. T. J. Chem. Ed. 2010, 87, 1348.

29 : “A Stereoselective Ring Expansion of Vinyl Oxiranes. Mechanistic Insights and Natural Product Total Synthesis” Brichacek, M.; Batory, L. A.; Njardarson, J. T. Angew. Chem. Int. Ed. 2010, 49, 1648.

28 : “A Concise Ring Expansion Route to the Compact Core of Platensimycin” McGrath, N. A.; Bartlett, E. S.; Sittihan, S.; Njardarson, J. T. Angew. Chem., Int. Ed. 2009, 48, 8543.

27 : “Rapid Assembly of Vinigrol’s Unique Carbocyclic Skeleton” Morton, J. G. M.; Dragichi, C.; Kwon, L. D.; Njardarson, J. T. Org. Lett. 2009, 11, 4492.

26 : “Creative Approaches Towards the Synthesis of 2,5-Dihydro- Furans, Thiophenes and Pyrroles. One Method Does Not Fit All!” Brichacek, M.; Njardarson, J. T. Org. Biomol. 2009, 7, 1761.

25 : “Efforts Towards the Total Synthesis of Vinigrol” Morton, J. G. M.; Kwon, L. D.; Freeman, J. D.; Njardarson, J. T. Synlett 2009, 23.

24 : “An Adler-Becker Oxidation Approach to Vinigrol” Morton, J. G. M.; Kwon, L. D.; Freeman, J. D.; Njardarson, J. T. Tetrahedron Lett. 2009, 50, 1684.

23 : “An Efficient Substrate Controlled Synthesis of Hypoestoxide, a Member of a Unique Family of Diterpenoid Natural Products with an Inside-Out [9.3.1]Bicyclic Core” McGrath, N.; Lee, C. A.; Araki, H.; Brichacek, M.; Njardarson, J. T. Angew. Chem. Int. Ed. 2008, 47, 9450.

22 : “Lewis Acid Catalyzed [1,3]-Sigmatropic Rearrangement of Vinyl Aziridines” Brichacek, M.; Njardarson, J. T.; Lee-D.-L. Org. Lett. 2008, 10, 5023.

21 : “PET Imaging of Soluble Yttrium-86-Labeled Carbon Nanotubes in Mice” McDewitt, M. R.; Chattopadhyay, D.; Jaggi, J. S.; Finn, R. D.; Zanzonico, P. B.; Villa, C.; Rey, D.; Mendenhall, J.; Batt, C. A.; Njardarson, J. T.; Scheinberg, D. A. PLoS One 2007, 2.
20 : “Tumor Targeting with Antibody-Functionalized Radiolabled Carbon Nanotubes” McDewitt, M. R.; Chattopadhyay, D.; Kappel, B. J.; Jaggi, J. S.; Schiffman, S. R.; Antczak, C.; Njardarson, J. T.; Brentjens, R.; Scheinberg, D. A. J. Nuc. Med. 2007, 48, 1180.
19 : “Highly Selective Copper-Catalyzed Ring Expansion of Vinyl Thiiranes: Application to Synthesis of Biotin and the Heterocyclic Core of Plavix®” Rogers, E.; Araki, H.; Batory, L. A.; McInnis, C. E.; Njardarson, J. T. J. Am. Chem. Soc. 2007, 129, 2768.

18 : “Copper Catalyzed Rearrangement of Vinyl Oxiranes” Batory, L. A.; McInnis, C. E.; Njardarson, J. T. J. Am. Chem. Soc. 2006, 128, 16054.

Type of Publication: graduate and post-doctoral publications
17 : “Confirmation of the Structure of Synthetic Derivatives of Migrastatin in the Light of Recently Disclosed Crystallographically Based Claims”Nagorny, P.; Krauss, I.; Njardarson, J. T.; Perez, L.; Gaul, G.; Yang, G.; Ouerfelli, O.; Danishefsky, S. J. Tetrahedron Lett. 2010, 51, 3873.
16 : “Synthetic Analogues of Migrastatin That Inhibit Mammary Tumor Metastasis in Mice” Shan, D.; Chen, L.; Njardarson, J. T.; Gaul, C.; Ma, X.; Danishefsky, S. J.; Huang, X.-Y. Proc. Natl. Acad. Sc.i U. S. A. 2005, 102, 3772.
15 : “The Migrastatin Family: Discovery of Promising Tumor Cell Migration Inhibitors by Chemical Synthesis” Gaul, C.; Njardarson, J. T.; Shan, D.; Dorn, D. C.; Wu, K.-D.; Tong, W. P.; Huang, X.-Y.; Moore, M. A.; Danishefsky, S. J. J. Am. Chem. Soc. 2004, 126, 11326.
14 : “Discovery of Potent Cell Migration Inhibitors through Total Synthesis: Lessons from Structure-Activity Studies of (+)-Migrastatin” Njardarson, J. T.’ Gaul, C.; Shan, D.; Huang, X.-Y.; Danishefsky, S. J. J. Am. Chem. Soc. 2004, 126, 1038.
13 : “Application of Phenolic Oxidation Chemistry in Synthesis: Preparation of the BCE Ring System of Ryanodine” Wood, J. L.; Graeber, J. K.; Njardarson, J. T. Tetrahedron 2003, 59, 8855.
12 : “Radicicol and the Epothilones: Total Synthesis of Novel Anti Cancer Agents Using Ring Closing Metathesis” Njardarson, J. T.; Garbaccio, R. M.; Danishefsky, S. J., in “Handbook of Metathesis”, Ed. Grubbs, Robert H.; Wiley, New York, 2003, Chapter 2.9, Appendix 3, p353.
11 : “Innovation and Art in Organic Chemistry: Synthetic Efforts Toward the Phomoidrides” Spiegel, D. A.; Njardarson, J. T.; McDonald, I.; Wood, J. L. Chem. Rev. 2003, 103, 2691.
10 : “The Total Synthesis of (+)-Migrastatin” Gaul, C.; Njardarson, J. T.; Danishefsky, S. J. J. Am. Chem. Soc. 2003, 125, 6042.
09 : “Application of Hitherto Unexplored Macrocyclization Strategies in the Epothilone Series: Novel Epothilone Analogs by Total Synthesis” Njardarson, J. T.; Biswas, K.; Danishefsky, S. J. Chem Commun. 2002, 2759.
08 : “Total Syntheses of [17]- and [18]Dehydrodesoxyepothilones B via a Concise Ring-Closing Metathesis-Based Strategy: Correlation of Ring Size with Biological Activity in the Epothilones Series” Rivkin, A.; Njardarson, J. T.; Biswas, K.; Chou, T-C.; Danishefsky, S. J. J. Org. Chem. 2002, 67, 7737.
07 : “Highly Concise Routes to Epothilones: The Total Synthesis and Evaluation of Epothilone 490” Biswas, K.; Lin, H.; Njardarson, J. T.; Chappell, M. D.; Chou, T.-C.; Guan, Y.; Tong, W. P.; He, L.; Horwitz, S. B.; Danishefsky, S. J. J. Am. Chem. Soc. 2002, 124, 9825.
06 : “CP-263,114 Synthetic Studies. Construction of an Isotwistane Ring System via Rhodium Carbenoid C-H Insertion” Spiegel, D. A.; Njardarson, J. T.; Wood, J. L. Tetrahedron 2002, 58, 6545.
05 : “Reactive Dienes: Intramolecular Aromatic Oxidation of 3-(2-Hydroxyphenyl)-propionic Acids” Drutu, I.; Njardarson, J. T.; Wood, J. L. Org. Lett. 2002, 4, 493.
04 : “An Expeditious Approach Towards the Total Synthesis of CP-263,114” Njardarson, J. T.; MacDonald, I.; Spiegel, D. A.; Inoue, M.; Wood, J. L. Org. Lett. 2001, 3, 2435.
03 : “Evolution of a Synthetic Approach to CP-263,114” Njardarson, J. T.; Wood, J. L. Org. Lett. 2001, 3, 2431.
02 : e Synthetic Route to Pure Isomers of the Antifungal Agents (E)- and (Z)-1,2-Diaryl-3-(1-imidazolyl)-1-propenes” Geirsson, J. K. F.; Gudmundsson, B. O.; Johannesdottir, J. F.; Njardarson, J. T.; Skulason, V. Acta Chem. Scand. 1995, 49, 423.
01 : “A Facile Synthesis of α-Phosphono Esters through Methoxycarbonylation of α-Phosphono Carbanions” Geirsson, J. K. F.; Njardarson, J. T. Tetrahedron Lett 1994, 35, 9071.
Type of Publication: Independent Patents
06 : “Single Wall Carbon Nanotube Constructs For Targeting Tumors” Scheinberg, D.; McDewitt, M.; Antczak, C.; Chattopahyay, D.; May, R.; Njardarson, J.; Phillips M. R.; PCT Int. Appl., (2007), WO 2007016466.
05 : “Process For the Preparation of 2,5-Dihydrofuran Derivatives” Njardarson, J. T.; Batory, L. A.; Bricachek, M.; Bauer, R. A.; Rogers, E. PCT Int. Appl., (2007), WO 2007108999.
Type of Publication: Patents From Post-Doctoral Work
04 :  “Preparation of Migrastatin and its Analogs for use in Pharmaceutical Compositions for the Treatment of Cancer” Danishefsky, S. J.; Gaul, C.; Njardarson, J. T., Moore, M. A. S.; Wu, K.; Dorn, D. C.; Mandal, M.; PCT Int. Appl., (2006), WO 2006001967.
03 : “Preparation of Migrastatin Analogs and their Biological Activity” Huang, X.-Y.; Danishefsky, S. J.; Gaul, C.; Njardarson, J. T.; PCT Int. Appl. (2004), WO 2004087672.
02 : “Preparation of Migrastatin Analogs and their Biological Activity” Danishefsky, S. J.; Gaul, C.; Njardarson, J. T.; PCT Int. Appl., (2004), WO 2004087673.
01 : “Synthesis of Epothilones for Therapeutic use as Anticancer Agents” Danishefsky, S. J.; Biswas, K.; Chappell, M. D.; Lin, H.; Njardarson, J. T.; Lee, C.; Rivkin, A.; Chou, T.-C. PCT Int. Appl. (2003), WO 2003022844.