Speaker: Ya Chen

Time: Friday, June 16, 2017, 16:00 p.m.

Location: 5#100 Conference Room

To modify lead compounds, modern medicinal chemists are increasing turning to unusual strained bioisosteres such as bicyclo[1.1.1]pentane, azetidine, and cyclobutane. However, the difficulty of installing these fragments often outweighs the challenge of synthesizing the parent scaffold itself. Recently, Phil S. Baran and co-workers have reported a general strategy where spring-loaded, strained C-C and C-N bonds react with nucleophiles to allow for the “any stage” installation of small, strained ring systems. The methodology has also been applied to peptide labeling and bioconjugation. In this report, I will introduce several strain-release reagents. More importantly, the development and application of strain-release heteroatom functionalization will be presented.

References

[1] Gianatassio, R.; Lopchuk, J. M.; Baran, P. S. et al. Science. 2016, 351, 241.

[2] Lopchuk, J. M.; Baran, P. S. et al. J. Am. Chem. Soc. 2017, 139, 3209.

[3] Dilmaç, A. M.; Bräse, S. et al. Angew. Chem. Int. Ed. 2017, 56, 2.

CURRICULUM VITAE

EDUCATION

2009-2013    Xiangtan University    B.S.

2013-2016    Xiangtan University    M.S.

2016-present  Institute of Chemistry, CAS    Ph.D. (Supervisor: Prof. Qing-Hua Fan)