Pharmaron Holds Eighth Annual Symposium on Synthetic and Medicinal Chemistry

Beijing China, September 15, 2018, Pharmaron held its 8th Symposium on Synthetic and Medicinal Chemistry.  Nine world-renowned professors and industry leaders from US, Europe, Japan and China, presented to hundreds of Pharmaron scientists and invited guests. The presenters discussed latest advancements in synthetic and medicinal chemistry, which included newly developed synthetic methodologies, total synthesis of highly complex natural products , design & synthesis of biologically active molecules, and the philosophy of innovation & team work.

Dr. Wendy Young from Genentech: Team work is an essential part of Genentech’s culture. Uniqueness and creativity of individuals are equally important. A small change can have a huge impact on discovery and development of small molecule drug candidates. Genentech, staff work hard, play hard.

Dr. Chengyi Chen from Janssen, emphasized the importance of understanding of reactions which could help develop innovative methodologies, and described the development of creative methodologies for N-O/N-N bonds formation based on the innovative indole  ring synthesis.

Prof. Biao Yu from SIOC, taking the total synthesis of complex natural Glycosides as an example, expounded the strategies and methods to solve the challenging problems: Scrutinizing analysis of phenomena leads to discovery of fundamental elements governing the phenomena.

Prof. Masakatsu Shibasaki  from Institute of Microbial Chemistry introduced the “team work” (cooperative catalysis) at molecular level. Using this concept, they developed different cooperative catalysts to catalyze a number of reactions in atom economic manner.

Dr. Jingjun Yin from MSD, said Chinese pronounce “research” as “Yan Jiu”, similar to that of “cigarette and alcohol”-common recreational substances. Dr. Yin said his research is his “cigarette and alcohol”. Dr. Yin introduced a methodology to simplify a reaction in water-containing condition. As a result, such reaction can be scaled up for industrial production and, at the same time, has minimum environmental impacts.

Dr. Tom Kinzel from Bayer (On behalf of Dr. Micheal Brands ), explores  the space of new targets by utilizing the diversity of compound structures, to achieve the goal of transforming the traditional un-drugable target  into a drugable.

Dr. Martin Eastgate from BMS emphasized the BMS approach to challenging chemistry problems, which is the disruptive innovation. This will start from novel chemistry which may derive from innovative  disconnection of organic molecules. This innovative disconnection will force the chemists to come up with novel  chemistry.

Dr. Frank Narjes from AstraZeneca described the discovery of an RORγt inverse agonist. By in-depth understanding and analysis of the interaction and the receptor, new interaction was identified, which improved potency and DMPK PROPOTIES. Now the optimized compound is in Phase I clinical trial.

Prof. Larry Overman from UC, Irvine, elaborated the strategy and tactics for the  total synthesis of complex natural products by utilizing tertiary carbon free-radicals. He has constructed a tertiary carbon structure with high stereo control through the reaction of tertiary carbon radicals, which greatly shortened the synthesis of natural products.

“This  is  a symposium on innovation which reflected the individual speaker, R&D team and company’s charters and styles of innovation philosophy and approach to problems. ” said Dr. Hua Yang, CSO at Pharmaron.