研究领域

主要从事新药研发、管理及商业转化，具体包括：新药合成工艺放大研究、工艺化学研发、催化在新药药化学的应用，跨部门新药研发管理，新兴市场研发战略制定、中国研发业务运营、研发商务拓展及许可等。

A direct asymmetric hydrogenation of unprotected enamino esters and amides is described. Catalyzed by Rh complexes with Josiphos-type chiral ligands, this method gives β-amino esters and amides in high yield and high ee (93−97% ee). No acyl protection/deprotection is required.

成果

创新性的将不对称氢化批量应用于如 Taranabant，Cordaptive®，首批 DPP-4 抑制剂 Januvia®，Belsomra® 等新药的生产合成路线，从而大幅提升了新药合成生产效率，有效减少了制造过程中产生的废料。Januvia® 的案例体现了显著的经济，环境和科学效益：基于崭新的不对称氢化的发明，API成本降低 70％；产生的废料量减少 80%；科研成果发表在化学顶尖杂志 JACS。

荣誉

• 2006 默克实验室最高奖 - 总裁奖

• 2005 英国化学工程师协会阿斯利康绿色化学与工程优秀奖

• 2005-2006 美国总统绿色化学挑战奖

• 2009 托马斯 - 爱迪生专利奖

• 2010 美国制药协会（PhRMA) “We Work for Health Champions”奖

• 2016 美国工程院院士

代表论文

1. Yi Hsiao*, Nelo R. Rivera*, Thorsten Rosner*, Shane W. Krska, Eugenia Njolito, Fang Wang, Yongkui Sun, Joseph D. Armstrong, Edward J. J., Grabowski, Richard D. Tillyer Felix Spindler, Christophe Malan. “Highly Efficient Synthesis of β-Amino Acids Derivatives via Asymmetric Hydrogenation of Unprotected Enamines”. Journal of the American Chemical Society. 2004. 126(32). 9918-9919 

2. Yongkui Sun, Ralph N. Landau, Jian Wang, Carl LeBlond, and Donna G. Blackmond*. “A Re-Examination of Pressure Effects on Enantioselectivity in Asymmetric Catalytic Hydrogenation”. Journal of the American Chemical Society. 1996. 118(6). 1348-1353. 

3. Karl B. Hansen*, Yi Hsiao*, Feng Xu*, Nelo Rivera, Andrew Clausen, Michele Kubryk, Shane Krska, Thorsten Rosner, Bryon Simmons, Jaume Balsells, Nori Ikemoto, Yongkui Sun, Felix Spindler, Christophe Malan, Edward J. J. Grabowski, and Joseph D. Armstrong III .“Highly Efficient Asymmetric Synthesis of Sitagliptin”. Journal of the American Chemical Society. 2009. 131(25), 8798-8804.

4. C. LeBlond, J. Wang, J. Liu, A. T. Andrews, and Y.-K. Sun* .“Highly Enantioselective Heterogeneously Catalyzed Hydrogenation of α-Ketoesters under Mild Conditions”. Journal of the American Chemical Society. 1999. 121(20). 4920-4921. 

5. Guohua Hou, Francis Gosselin*, Wei Li, J. Christopher, McWilliams, Yongkui Sun, Mark Weisel, Paul D. O’Shea, Cheng-yi Chen, Ian W. Davies, Xumu Zhang* . “Enantioselective Hydrogenation of N-H Imines”. Journal of the American Chemical Society. 2009. 131(29). 9882-9883.