研究成果

研究成果

 

Papers:

1. “The Development and Manufacture of Azacitidine, Decitabine, and Cladribine: Stereoselective Ribonucleoside Drug Synthesis Using the Vorbrüggen Glycosylation”, Erick W. Co and J. P. Henschke*, Comprehensive Accounts of Drug Research and Development: From Discovery to Late Development and Beyond, Volume 2, Chapter 9, pp 271–321; Edited by J. Pesti, A. Abdel-Magid and R.Vaidyanathan, ACS Books, in press (published online 9th Dec., 2016: chapter DOI: 10.1021/bk-2016-1240.ch009).

2. "Rh(I)-Catalyzed 1,4-Conjugate Addition of Alkenylboronic Acids to a Cyclopentenone Useful for the Synthesis of Prostaglandins", Jin-Fong Syu, Yun-Ting Wang, Kung-Cheng Liu, Ping-Yu Wu, Julian P. Henschke, and Hsyueh-Liang Wu, Journal of Organic Chemistry 2016, 81, 10832–10844. DOI: 10.1021/acs.joc.6b01913.

3. “Rhodium-Catalyzed Enantioselective Arylation of N-Substituted α,β-Unsaturated γ-Lactams: Preparation of Chiral 4-Aryl-2-Pyrrolidones", Fang, J.-H., Chang, C.-A., Gopula, B., Kuo, T.-S., Wu, P.-Y., Henschke, J. P. and Wu, H.-L., Asian J. org. Chem. 2016, 5, 481-485.

4. “Direct Synthesis of Chiral 3-Arylsuccinimides by Rhodium-Catalyzed Enantioselective Conjugate Addition of Arylboronic Acids to Maleimides”, Balraj Gopula, Shu-Han Yang, Ting-Shen Kuo, Jen-Chieh Hsieh,* Ping-Yu Wu, Julian P. Henschke,* and Hsyueh-Liang Wu,* Chemistry, A European Journal 2015, 21, 11050–11055; “Hot Paper” and featured on back cover of issue 31.

5. “β Selective C-Arylation of Diisobutylaluminum Hydride Modified 1,6-Anhydroglucose: Synthesis of Canagliflozin without Recourse toConventional Protecting Groups”, Julian P. Henschke, Chen-Wei Lin, Ping-Yu Wu, Wen-Shing Tsao, Jyh-Hsiung Liao and Pei-Chen Chiang, J. Org. Chem. 2015, 80 , 5189-5195.

6. “Rhodium/Chiral Diene Complexes in the Catalytic Asymmetric Arylation of β Pyrazol-1-yl Acrylates”, Balraj Gopula, Yun-Fan Tsai, Ting-Shen Kuo, Ping-Yu Wu, Julian P. Henschke and Hsyueh-Liang Wu, Org. Lett. 2015, 17, 1142-1145.

7. “β Selective C Arylation of Silyl Protected 1,6-Anhydroglucose with Arylalanes: The Synthesis of SGLT2 Inhibitors”, Julian P. Henschke, Ping-Yu Wu, Chen-Wei Lin, Shi-Feng Chen, Pei-Chen Chiang and Chi-Nung Hsiao, J. Org. Chem. 2015, 80, 2295–2309.

8. “Enantioselective and Rapid Rh-Catalyzed Arylation of N-Tosyl- and N-Nosylaldimines in Methanol”, Chun-Chih Chen, Balraj Gopula, Jin-Fong Syu, Jhih-Han Pan, Ting-Shen Kuo, Ping-Yu Wu, Julian P. Henschke, and Hsyueh-Liang Wu, J. Org. Chem. 2014, 79, 8077−8085.

9. “Highly Enantioselective Rh-Catalyzed Alkenylation of Imines: Synthesis of Chiral Allylic Amines via Asymmetric Addition of Potassium Alkenyltrifluoroborates to N Tosyl Imines”, Balraj Gopula, Chien-Wei Chiang, Way-Zen Lee, Ting-Shen Kuo, Ping-Yu Wu, Julian P. Henschke, Hsyueh-Liang Wu, Org. Lett. 2014, 16, 632−635. This paper was cited in “Highlights in Current Synthetic Organic Chemistry”, Synfacts 2014, 10, 0395.

10. “Rhodium-Catalyzed Asymmetric Addition of Arylboronic Acids to β-Nitroolefins: Formal Synthesis of (S)-SKF 38393”, Kung-Chih Huang, Balraj Gopula, Ting-Shen Kuo, Chien-Wei Chiang, Ping-Yu Wu, Julian P. Henschke, Hsyueh-Liang Wu, Org. Lett. 2013, 15, 5730–5733. This paper was cited in “Highlights in Current Synthetic Organic Chemistry”, Synfacts 2014, 10, 0180.

11. “A Stereoselective Process for the Manufacture of a 2’-Deoxy-β D Ribonucleoside Using the Vorbrüggen Glycosylation”, Julian P. Henschke, Xiaoheng Zhang, Xiaohong Huang, Lijun Mei, Guodong Chu, Kun Hu, Qingping Wang, Guoyang Zhu, Mingfeng Wu, Chihying Kuo, Yungfa Chen, Org. Process Res. Dev. 2013, 17, 1419−1429.

12. “Synthetic Process Development of BMS-599793 Including Azaindole Negishi Coupling on Kilogram Scale”, Stanislaw Pikul, Hua Cheng, Allen Cheng, C. D. Huang, Alex Ke, LungHuang Kuo, Andrew Thompson, and Susan Wilder Org. Process Res. Dev. 2013, 17, 907−914.

13. “A global comparability approach for biosimilar monoclonal antibodies using LC–tandem MS based proteomics”, Shun-Li Chen, Shiaw-Lin Wu, Li-Juan Huang, Jia-Bao Huang, Shu-Hui Chen J. Pharm. Biomed. Anal. 2013, 80, 126–135.

14. “Structural stability-chromatographic retention relationship on exenatide diastereomer separation” Ching-Wei Tsai, Wei-Hung Kao, Li-Chiao Chang, Ruoh-Chyu Ruaan and Wen-Yih Chen Anal. Bioanal. Chem. 2012, 404, 2437-2444.

15. “The manufacture of a homochiral 4-silyloxycyclopentenone intermediate for the synthesis of prostaglandin analogues”, Julian P. Henschke, Yuanlian Liu, Xiaohong Huang, Yungfa Chen, Dechao Meng, Lizhen Xia, Xiuqiong Wei, Aiping Xie, Danhong Li, Qiang Huang, Ting Sun, Juan Wang, Xuebin Gu, Xinyan Huang, Longhu Wang, Jun Xiao, Shenhai Qiu, Org. Process Res. Dev. 2012, 16, 1905−1916.

16. “Micronization of Fluticasone Propionate using Supercritical Antisolvent Process”, Chie-Shaan Su, Wei-Shuo Lo, Ling-Hsiao Lien, Chem. Eng. Technol. 2011, 34, 535–541.

17. “Recrystallization of erlotinib hydrochloride and fulvestrant using supercritical antisolvent process“, Yao-Chun Tien, Chie-Shaan Su, Ling-Hsiao Lien, Yan-Ping Chen J. of Supercritical Fluids 2010, 55, 292–299.

18. “Convergent Solution Phase Synthesis of Chimeric Oligonucleotides by a 2+2 and 3+3 Phosphoramidite Strategy”, Chen, C.-H.; Chen, W.-Y.; Chen, Y.-C.; Lee, M-J.; Huang, C.-D.; Chanda, K.; Sun, C.-M. Aust. J. Chem. 2010, 63, 227–235.

19. “Identification and Suppression of a Dimer Impurity in the Development of Delafloxacin”, Roger Hanselmann, Graham Johnson, Maxwell M. Reeve, and Shu-Ting Huang Org. Process Res. Dev. 2009, 13, 54–59.

 

Presentations:

1. “Highly β-Selective C-Arylation of 1,6-Anhydroglucose:Synthesis of SGLT2 Inhibitors”, Julian P. Henschke, The 11th International Symposium on Organic Reactions, Taipei, Taiwan, November 20th, 2013.

2. “Process Development of Fondaparinux Sodium”, Lung-Huang Kuo, The 9th AFMC International Medicinal Chemistry Symposium, Taipei, Taiwan, October 16th, 2013.

3. “Simultaneous Analysis of Acetamide and Pyridine in Pharmaceutical Samples by GC-MS”, I-Min Huang, The 19th Annual Conference for Technical Communication on Analytical Chemistry, Taipei, Taiwan, May 25th, 2013.

4. “Analysis of poly-sulfated oligosaccharide using hydrophilic interaction chromatography charged aerosol detector”, Chung-Yao, Wang, The 19th Annual Conference for Technical Communication on Analytical Chemistry, Taipei, Taiwan, May 15th, 2013.

5. “Use of the Suzuki-Miyaura Cross-Coupling Reaction in a Key Step in the Synthesis of a Kinase Inhibitor”, Julian P. Henschke, 7th International BASF Boron Conference, November 10th , 2011, Tokyo, Japan.

 

Posters:

1. “Highly β-Selective C-Arylation of 1,6-Anhydroglucose:Synthesis of SGLT2 Inhibitors” J. P. Henschke, Ping-Yi Wu, Chen-wei Lin, Shi-Feng Chen and Jyh-Hsiung Liao, Annual Meeting of Chemical Society Located in Taipei, National Chi Nan University, Puli, Nantou county, Taiwan, 23rd November, 2013.

2. “Quantitation of Melamine in Pharmaceutical Samples using LC-MS/MS” Hsien-Chang Su , Annual Meeting of Chemical Society Located in Taipei, National Chi Nan University, Puli, Nantou county, Taiwan, 23rd November, 2013.

3. “Rearrangement structure identification of Exemestane process impurity by MS and NMR” Yu-Hui Chen, Hsien-Chang Su, Chi-Hsien Lin and Long-Hu Wang, Annual Meeting of Chemical Society Located in Taipei, National Chi Nan University, Puli, Nantou county, Taiwan, 23rd November, 2013.

4. “Using online multiple SPE system coupled with ESI/MS to automatically establish LC impurity profile in pharmaceutical industry”, Chi-Hsien Lin, Hsien-Chang Su, Lung-Cheng Lin, The 4th Asia Oceania Mass Spectrometry Conference and 10th Taiwan Society for Mass Spectrometry Annual Conference, Taipei, Taiwan, July 10th~12th, 2013.