Faculty |
Jian WANG, Ph.D.

Jian WANG, PI, Tenured Full Professor

Professor Wang joined School of Pharmaceutical Sciences, Tsinghua University (Beijing, China) in December 2012. Prior to that, he held position of Assistant Professor (tenure-track) in the Department of Chemistry at National University of Singapore (Singapore) from 2009 to 2012. Professor Wang obtained his Ph.D. in Chemistry from University of New Mexico (Albuquerque, NM, USA) in 2007, and his undergraduate education degree (1997) from the Department of Chemistry, Anhui Normal University, Anhui, China. He has been invited to give presentations in many domestic or international conferences, and has severed as reviewers for many peer-reviewed chemistry/pharmaceutical journals. So far, he has published> 100 peer reviewed papers and 8 patents. Prof. Wang also served as the Chief Editor of Journal of Natural Products Against Cancer.


Research interests 

1)Development of innovative chemical synthesis tools for drug candidate modification or drug synthesis

2) Targeted therapy for cancers

3) First-in-class (concept) novel drug development for neurodegenerative diseases (AD, PD, etc)

3)N-Heterocyclic carbene asymmetric catalysis



Selected Achievements

1. With respect to industrial applications, organocatalytic reactions are of great use to medicinal chemists. These researchers are the largest body of industrial synthetic chemists in the world, and their technological needs often differ from those of chemists in manufacturing or process development. Medicinal chemists need to find rapid, broadly applicable ways of constructing new candidate drugs for testing, so the most important considerations for a catalyst are its generality, convenience and robustness. Organocatalysts meet all of these operational requirements. Indeed, organocatalysts have already been taken up by some medicinal chemists in pursuit of therapeutic agents enriched for a particular enantiomer. To our knowledge, the development of novel synthetic method for the construction of a unique library of heterocycles or organofluoro compounds is of great significance for drug (screening) discovery. Our group herein devoted to disclose novel methods to construct biologically or medicinally important compounds.

2. The use of small organic molecules to catalyze organic transformations is a relatively new and popular field. Although chemical transformations that use organocatalysts have been documented sporadically over the past century, the application of such concept in heterocyclic synthesis is still highly desirable. As indicated in Figure below, out team utilized the in situ generated enamines to react with various 1,3-dipoles to efficiently generate a diverse set of synthetic useful heterocycles, e.g. 1,2,3-triazoles, pyrazoles, isoxazoles, etc. In these processes, cheap amines were used as active organocatalysts.


3. The continually increasing challenges associated with the treatment of new and existing diseases necessitates that potential therapeutics contain higher levels of molecular complexity to achieve potency, selectivity and desirable physical properties. Of particular relevance is the emergence of drug candidates with one or more non-racemic, asymmetric centres. Single-enantiomer drugs are, however, significantly more difficult to synthesize using conventional asymmetric synthesis; new enantioselective methods are thus required to meet this challenge. Enantioselective organocatalysis has now emerged as a powerful synthetic paradigm and has accelerated the development of new methods to make diverse chiral molecules. As indicated in Figure below, we successfully disclosed our indane-structure based bifunctional amine-thiourea catalytical system. Notably, these unique indane catalysts resulted in several important transformations in combination with excellent enantio- and diastero-control. The generated chiral scaffolds are of great importance in medicinal chemistry and drug discovery.


4. Divergent catalytic reactions provide quick access to structurally different compounds from a common precursor through controlled reaction pathways, and are highly attractive tools in the discovery of drugs and functional materials. A more promising, yet challenging strategy that remains largely unexplored is tandem divergent catalysis, which combines the key advantages inherent to both tandem reactions and divergent catalysis to provide a rapid access to different structures from the same simple reagents while minimizing the generation of waste. In the course of our studies on the tandem use, herein, we report a few strategies based on divergent palladium catalysis that provides a number of distinct heterocyclic scaffolds


5. The identification of pharmacological agents that control adult or embryonic stem cell fate has the potential to facilitate the application of stem cell therapies to a host of diseases. 1) Although practiced clinically for more than 40 years, the use of hematopoietic stem cell (HSC) transplants remains limited by the ability to expand these cells ex vivo. An unbiased screen with primary human HSCs identified a purine derivative, StemRegenin 1 (SR1), that promotes the ex vivo expansion of CD34+ cells. Culture of HSCs with SR1 led to a 50-fold increase in cells expressing CD34 and a 17-fold increase in cells that retain the ability to engraft immunodeficient mice; 2) Embryonic stem cells (ESCs) are an attractive source of cells for disease modeling in vitro and may eventually provide access to cells/tissues for the treatment of many degenerative diseases. Using a high-content screen, we have identified a small molecule, named stauprimide, that increases the efficiency of the directed differentiation of mouse and human ESCs in synergy with defined extracellular signaling cues


6. Development of new drugs for the treatment of Alzheimer's disease based on the "forgetting mechanism": The applicant team and the team of Professor Zhong Yi, a neuroscience expert at the School of Life Sciences of Tsinghua University, combined with the in-depth understanding gained from years of studying the brain, have opened up another way to use the forgetting mechanism as a new breakthrough in the development of Alzheimer's disease, and to develop drugs that inhibit accelerated forgetting by identifying forgetting molecules, with a view to improving Alzheimer's disease from the memory level. At present, the development of new drugs (first-in-class) for Alzheimer's disease (AD) has been approved by CDE, and clinical research has been carried out in Xuanwu, Xiehe and other hospitals



Honors and awards

The Leading Talents of the National Ten Thousand Talents Program (2021)

Young and Middle-aged Innovative Scientific and Technological Talents of the Ministry of Science and Technology (2020)

The One Thousand Talent Program Young Scholar (2012)

Bayer Investigator Award (2015)

OCF Emerging Investigator(2015, RSC)

Editor of Natural Products Against Cancer(2012-2014)

Asia Core Program Lectureship(Japan, 2013)

Asia Core Program Lectureship(China, 2013)

Nanyang Assistant Professorship (2009)

NUS Assistant Professorship (2009)

Excellent Chinese Self-financed Oversea Student Award (2006, USA)

Sigma Xi Research Award (2007)

Distinguished Ph.D of University of New Mexico (2007)


Selected publications 

1.Li, L. Y.; Wang, X.; Gao, R.; Zhang, B.; Liu, Y.; Zhou, J.; Fu, L.; Wang, J*; Inflammation-Triggered Supramolecular Nanoplatform for Local Dynamic Dependent Imaging-Guided Therapy of Rheumatoid Arthritis,Adv. Sci., 2022, 2105188.

2.Peng, Q.; Yan, B..; Li, F.; Lang, M.; Zhang, B.; Guo, D.; Bierer, D.; Wang, J*; Biomimetic Enantioselective Synthesis of β,β-Difluoro-α-amino Acid Derivatives,Commun. Chem., 2021, 4, 148.

3.Li, L.; Zhang, B.; Liu, Y.; Gao, R.; Zhou, J.; Fu, L.; Wang, J*; A Spontaneous Membrane-Adsorption Approach to Enhancing Second Near-Infrared Deep-Imaging-Guided Intracranial Tumor Therapy,ACS Nano, 2021, 15, 4518.

4.Yang, G. M.; Guo, D. H.; Meng, D.; Wang, J*; NHC-catalyzed Atropoenantioselective Synthesis of Axially Chiral Biaryl Amino Alcohols via a Cooperative Strategy,Nature Commun., 2019, 10, 3062.

5.Zhao, C. G;Guo, D. H.; Munkerup, K.; Huang, K. W.; Li, F. Y.; Wang, J*; Enantioselective [3+3] Atroposelective Annulation Catalyzed by N-heterocyclic Carbenes,Nature Commun., 2018, 9, 611.

6.Peng, Q. P.; Guo, D. H.; Bie, J. B.; Wang, J*; Catalytic Enantioselective Aza‐Benzoin Reactions of Aldehydes with 2H‐Azirines, Angew. Chem. Int. Ed., 2018, 57, 3761.

7.Zhang, J. W.; Wang, J*; Atropoenantioselective Redox‐Neutral Amination of Biaryl Compounds through Borrowing Hydrogen and Dynamic Kinetic Resolution, Angew. Chem. Int. Ed., 2018, 57, 465.

8.Wu, Z. J.; Wang, J*; A Tandem Dearomatization/Rearomatization Strategy: Enantioselective N-Heterocyclic Carbene-Catalyzed α-Arylation, Chem. Sci., 2019, 10, 2501.

9.Wu, J. C.; Zhao, C. G.; Wang, J*; Enantioselective Intermolecular Enamide-Aldehyde Cross-Coupling Catalyzed by Chiral N-Heterocyclic Carbenes, J. Am. Chem. Soc., 2016, 138, 4706.

2. Zhao, C. G.; Li, F. Y.; Wang, J*; N-heterocyclic Carbene Catalyzed Dynamic Kinetic Resolution of Pyranones, Angew. Chem. Int. Ed., 2016, 55, 1820.

10.Zhao, C. G.; Li, F. Y.; Wang, J*; N-heterocyclic Carbene Catalyzed Dynamic Kinetic Resolution of Pyranones, Angew. Chem. Int. Ed., 2016, 55, 1820.

11.Wu, J. C.; Xu, W. B.; Yu, Z.-X.*; Wang, J*; Ruthenium-catalyzed Formal Dehydrative [4 + 2] Cycloaddition of Enamides and Alkynes for the Synthesis of Highly Substituted Pyridines: Reaction Development and Mechanistic Study, J. Am. Chem. Soc., 2015, 137, 9489.

12.Wu, Z. J.; Li, F. Y.; Wang, J*; Intermolecular Dynamic Kinetic Resolution Cooperatively Catalyzed by an N-Heterocyclic Carbene and a Lewis Acid, Angew. Chem. Int. Ed., 2015, 54, 1629.

13.Li, F. Y.; Wu, Z. J.; Wang, J*; Oxidative Enantioselective α-Fluorination of Aliphatic Aldehydes Enabled by N-Heterocyclic Carbene Catalysis, Angew. Chem. Int. Ed., 2015, 54, 656.

14.Li, W. J.; Wang, J*; Lewis Base Catalyzed Aerobic Oxidative Intermolecular Azide-Zwitterion Cycloaddition, Angew. Chem. Int. Ed., 2014, 53, 14186.

15.Wang, L.; Huang, J. Y.; Liu, H.; Peng, S. Y.; Jiang, X.-F.*; Wang, J.* Palladium-catalyzed Oxidative Cycloaddition via C–H/N–H Activation: Access to Benzazepines, Angew. Chem. Int. Ed., 2013, 52, 1768.

16.Boitano, A. E.; Wang, J.; Romeo, R.; Bouchez, L. G.; Parker, A. E; Sutton, S. U.; Walker, J. R.; Flaveny, C. A.; Perdew, G. H; Denison, M. S.; Schultz, P. G., Cooke, M. P. Aryl Hydrocarbon Receptor Antagonists Promote the Expansion of Human Hematopoietic Stem Cells, Science 2010, 329, 1345-1348.

17.Zhu, S. T.; Wurdak, H.; Wang, J.; Lyssiotis, C. A.; Peters, E. C.; Cho, C. Y.; Wu, X.; Schultz, P. G. A Small Molecule Primes Embryonic Stem Cells for Differentiation, Cell Stem Cell, 2009, 4(5), 416-426.

18.Wang, J.; Xie, H.-X.; Li, H.; Zu, L.-S.; Wang, W. A Highly Stereoselective Hydrogen-Bond-Mediated Michael-Michael Cascade Process through Dynamic Kinetic Resolution, Angew. Chem. Int. Ed., 2008, 47, 4177.

19.Wang, J.; Li, H.; Zu, L.-S.; Wang, W. Organcatalytic Enantioselective Conjugate Additions to Enones, J. Am. Chem. Soc., 2006, 128, 12652.

20.Wang, J.; Li, H.; Xie, H.-X.; Zu, L.-S.; Shen, X.; Wang, W. Organocatalytic Enantioselective Cascade Michael-Aldol Condensation Reactions: Efficient Assembly of Densely Functionalized Chiral Cyclopentenes, Angew. Chem. Int. Ed., 2007, 46, 9050.

21.Wang, J.; Li, H.; Wang, W.; Direct, Highly Enantioselective Pyrrolidine Sulfonamide Catalyzed Michael Addition Reactions of Aldehydes to Nitrostyrenes, Angew. Chem. Int. Ed., 2005, 44, 1369.


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