报告题目：New Synthetic Methodologies Promoting Drug Discovery

报 告 人：林华（美国斯克里普斯研究所）

报告时间：2019年6月5日（星期三）14:00

报告地点：药学院云轩楼1323会议室

报告人简介：

Dr Hua Lin received B.S, M.S and Ph.D From Fudan University under the supervision of Prof. Guoqiang Lin. His research is aimed at 1) developing methodologies for the synthesis of chiral building blocks which are useful for total synthesis of natural products and bioactive compounds; and 2) design and synthesis of bioactive compounds discovered through sophisticated Structure-Activity Relationship studies at the molecular level. Which were target at nuclear receptors, such as ERRα, ERRβ, ERRγ, PGC1α, PPARγ, Rev-erb for the treatment of type 2 diabetes and obesity.

报告摘要：

New synthetic methodologies have been developed for the synthesis of nitrogen-containing compounds, including 1) The first selective Pd-catalysed γ-C(sp3)-H and γ-C(sp2)-H arylation of free amino esters using a commercially available catalytic transient directing group; 2) A Pd(II)-catalyzed, selective δ-C(sp3)−H and δ-C(sp2)−H arylation method for free primary aliphatic amines using NH2 as a native directing group; 3) A three or four-component asymmetric cascade reaction for the construction of chiral tetrahydro-1,2-oxazine derivatives or tetrahydropyridines in high yields with excellent diastereoselectivities. Then the new C-H activation reactions have been applied for the design and synthesis of divergent N-Acyl amino acids. The administration of N-acyl amino acids to mice improves glucose homeostasis and increases energy expenditure, indicating that this pathway might be useful for treating obesity and associated disorders.