Middle Molecular Strategy

Part I: Development of bio-functional middle molecules.- 1. Introduction.- 2. Total Synthesis, Biological Evaluation and 3D Structural Analysis of Cyclodepsipeptide Natural Products.- 3. Development of the Middle-size Molecules for Alkylation to Higher-Order Structures of Nucleic Acids.- 4. In Situ Synthesis of Glycoconjugates on Cell Surface: Selective Cell Imaging Using Low-Affinity Glycan Ligands.- 5. Assembled mid-sized agents that control intracellular protein-protein interactions.- 6. Macrocyclic mid-sized peptides with new chemical modalities.- Part II: Achievement of highly efficient synthesis of bioactive middle molecules.- 7. Enantioselective Total Synthesis of Cotylenin.- 8. Flow Chemistry for the Construction of Polycyclic Skeleton.- 9. Electrochemical Synthesis of Oligosaccharides as Middle-sized Molecules.- 10. Efficient Synthesis of Biologically Active Peptides based on Micro-flow Amide Bond Formation.- 11. Design and Concise De Novo Synthesis of Artemisinin Analogs.

Koichi Fukase graduated from the Department of Chemistry, Osaka University, in 1982 and received his Ph.D. from Osaka University (under Prof. Tetsuo Shiba) in 1987. After spending 1 year as a JSPS Postdoctoral Fellow (under Prof. Shiba), he was appointed as Assistant Professor (1988-1996) at the Department of Chemistry, School of Science, Osaka University (under Prof. Shoichi Kusumoto). In 1994, he joined Prof. W. Clark Still's group at Columbia University as a Ministry of Education Research Fellow. After returning to Osaka in 1995, he was promoted to Lecturer (1996) and Associate Professor (1998) and became Full Professor at the Department of Chemistry, Graduate School of Science, Osaka University, in 2004. He received the Chemical Society of Japan Award for Creative Work in 2011. His research interests include carbohydrate chemistry and glycobiology, synthetic organic chemistry, bio-imaging, and innate immunity.

Takayuki Doi received his Ph.D. from Tokyo Techin 1991 (under Prof. Takashi Takahashi). After a postdoctoral scientist position under Prof. Gilbert Stork at Columbia University, he joined Tokyo Tech as Assistant Professor in 1993 and became Associate Professor in 2001. He was promoted to Full Professor at the Graduate School of Pharmaceutical Sciences, Tohoku University, in 2008 and joined the Graduate School of Life Sciences in 2018. He received the Progress Award in Synthetic Organic Chemistry, Japan in 2000, and the Pharmaceutical Society of Japan Award for Divisional Scientific Promotions in 2013.