化学所分子识别与功能实验室
学术带头人

       俞初一  研究员

       

        中国科学院“百人计划”入选者

        电话:86-10-62612893

        传真:86-10-62612893

        邮箱:yucy@iccas.ac.cn;

        课题组主页:http://yucy.iccas.ac.cn/

     

    学术经历

    1989-1992   中国科学院化学研究所硕士学位

    1992-1995   中国科学院化学研究所博士学位

    1995-1996   中国科学院化学研究所助研

    1996-1999   英国桑德兰大学博士后

    1999-2001   英国牛津大学博士后

    2001-至今    中国科学院化学研究所,研究员

     

    荣誉与奖项

    2001年   入选中国科学院“百人计划”

     

    研究方向

    1. 天然产物合成化学

    以一些结构新颖或具有重要生物活性的亚氨基糖为合成目标,发展简洁、高效的合成方法,目前已经完成了一系列重要天然产物及其对映体的合成工作,包括Radicame A、B、(-)-Hyacinthacine C5、Steviamine、 Australine、Unifluorine A、(-)-Erycibelline、Broussonetine I、J、J1、J2、W、M、S、Pochonicine、Calystegines B2、B3等。

    2. 糖化学生物学

    针对一些具有重要生物活性的亚氨基糖,设计、合成其类似物,开展生物活性评价、系统研究其构效关系,在此基础上设计、合成新的先导化合物。

    3. 高效的药物合成技术研究

    针对 DNJ、米格列醇、普拉克素等重要药物,开展其及关键中间体的高效合成技术研究。目前,部分研究成果已进入GMP生产阶段、部分研究成果正在进行中试放大研究。

     

    Selected Work

    1. Synthesis and biological activities of polyhydroxylated alkaloids

     

    2. Total synthesis and biological activities of broussonetine I and J2

     

    3. Total synthesis and biological activities of pochonicine and its analogs

     

     

    4. Synthesis and biological activities of australine and its fluorinated derivatives

     

    5. Concise synthesis of calystegines B2 and B3 via intramolecular NHK reaction

     

    Selected Publications

    1. Li, Y. X.; Iwaki, R.; Kato, A.*; Jia, Y. M.; Fleet, G. W. J.; Zhao, X.; Xiao, M.; Yu, C. Y.*, “Fluorinated Radicamine A and B: Synthesis and Glycosidase Inhibition”Eur. J. Org. Chem. 2016, (7), 1429-1438.

    2. Li, Y. X.; Kinami, K.; Hirokami, Y.; Kato, A.*; Su, J. K.; Jia, Y. M.; Fleet, G. W. J.; Yu, C. Y.*“Gem-difluoromethylated and trifluoromethylated derivatives of DMDP-related iminosugars: synthesis and glycosidase inhibition” Org. Biomol. Chem. 2016, 14 (7), 2249-2263.

    3. Qian, B. C.; Kamori, A.; Kinami, K.; Kato, A.*; Li, Y. X.; Fleet, G. W. J.; Yu, C. Y.* “Epimerization of C5 of an N-hydroxypyrrolidine in the synthesis of swainsonine related iminosugars” Org. Biomol. Chem. 2016, 14 (19), 4488-4498.

    4. Song, Y. Y.; Kinami, K.; Kato, A.*; Jia, Y. M.; Li, Y. X.; Fleet, G. W. J.; Yu, C. Y.* “First total synthesis of (+)-broussonetine W: glycosidase inhibition of natural product & analogs” Org. Biomol. Chem. 2016, 14 (22), 5157-5174.

    5. Wang, H. Y.; Kato, A.*; Kinami, K.; Li, Y. X.; Fleet, G. W. J.; Yu, C. Y.* “Concise synthesis of calystegines B-2 and B-3 via intramolecular Nozaki-Hiyama-Kishi reaction” Org. Biomol. Chem. 2016, 14 (21), 4885-4896.

    6. Li, Y.-X.; Shimada, Y.; Sato, K.; Kato, A.*; Zhang, W.; Jia, Y.-M.; Fleet, G. W. J.; Xiao, M.; Yu, C.-Y.*, “Synthesis and Glycosidase Inhibition of Australine and Its Fluorinated Derivatives” Org. Lett. 2015, 17 (3), 716-719.

    7. Li, Y.-X.; Shimada, Y.; Adachi, I.; Kato, A.*; Jia, Y.-M.; Fleet, G. W. J.; Xiao, M.; Yu, C.-Y*., “Fluorinated and Conformationally Fixed Derivatives of L-HomoDMDP: Synthesis and Glycosidase Inhibition.” J. Org. Chem. 2015, 80 (10), 5151-5158.

    8. Zhu, J.-S.; Nakagawa, S.; Chen, W.; Adachi, I.; Jia, Y.-M.; Hu, X.-G.; Fleet, G. W. J.; Wilson, F. X.; Nitoda, T.; Horne, G.; van Well, R.; Kato, A.*; Yu, C.-Y.*, “Synthesis of Eight Stereoisomers of Pochonicine: Nanomolar Inhibition of β-N-Acetylhexosaminidases.” J. Org. Chem. 2013, 78, 10298-10309.

    9. Zhao, H.; Kato, A.; Sato, K.; Jia, Y. M.; Yu, C. Y., “Total Synthesis and Glycosidase Inhibition of Broussonetine I and J2.” J. Org. Chem. 2013, 78 (16), 7896-7902

    10. Zhao, W.-B.; Nakagawa, S.; Kato, A.; Adachi, I.; Jia, Y.-M.; Hu, X.-G.; Fleet, G. W. J.; Wilson, F. X.; Horne, G.; Yoshihara, A.; Izumori, K.; Yu, C.-Y.* “ General Synthesis of Sugar-Derived Azepane Nitrones: Precursors of Azepane Iminosugars” J. Org. Chem. 2013 78, 3208-3221.

    11. Zhang, Z.-L.; Nakagawa, S.; Kato, A.; Jia, Y.-M.; Hu, X.-G.; Yu, C.-Y.* “A concise stereoselective synthesis of (-)-erycibelline” Org. Biomol. Chem. 2011, 7713-7719.( hot paper)

    12. Zhang, W.; Sato, K.; Kato, A.; Jia, Y.-M.; Hu, X.-G.; Wilson, F. X.; van Well, R.; Horne, G.; Fleet, G. W. J.; Nash, R. J.; Yu, C.-Y.* “Synthesis of fully substituted polyhydroxylated pyrrolizidines via Cope-House cyclization” Org. Lett. 2011, 13, 4414-4417.

    13. Li, Y. X.; Huang, M. H.; Yamashita, Y.; Kato, A.; Jia, Y. M.; Wang, W. B.; Fleet, G. W. J.; Nash, R. J.; Yu, C. Y.* “L-DMDP, L-homoDMDP and their C-3 fluorinated derivatives: Synthesis and glycosidase-inhibition” Org. Biomol. Chem. 2011, 9, 3405-3414.

    14. Hu, X.-G.; Bartholomew, B.; Nash, R. J.; Wilson, F. X.; Fleet, G. W. J.; Nakagawa, S.; Kato, A.; Jia, Y.-M.; Well, R. V.; Yu, C.-Y.* “Synthesis and glycosidase inhibition of the enantiomer of (-)-steviamine, the first example of a new class of indolizidine alkaloid” Org. Lett. 2010, 12, 2562-2565.

    15. Wang, W.-B.; Huang, M.-H.; Li, Y.-X.; Rui, P.-X.; Hu, X.-G.; Zhang, W.; Su, J.-K.; Zhang, Z.-L.; Zhu, J.-S.; Xu, W.-H.; Xie, X.-Q; Jia Y.-M.;* Yu, C. Y.* “A practical synthesis of sugar-derived cyclic nitrones: Powerful synthons for the synthesis of iminosugars” Synlett 2010, 488-492.

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