Organic Chemistry: Current Research
Open Access
ISSN: 2161-0401
+44 1478 350008
ISSN: 2161-0401
+44 1478 350008
Bryan Li
Pfizer Inc.-Groton, USA
Scientific Tracks Abstracts: Organic Chem Curr Res
Alzheimer’s disease (AD) is widely believed to be related to the production and deposition of the beta-amyloid (Aβ). Thus, beta-amyloid cleaving enzyme (BACE1) inhibitors, that can reduce the production of the Aβ peptide, are promising candidates for the treatment of AD. Pfizer researchers discovered a potent, selective BACE1 inhibitor that displayed good safety, tolerability, and pharmacokinetics from early stage clinical trials. The compound also exhibited excellent brain penetration, and potent in vivo efficacy. The exploratory active pharmaceutical ingredient (API) support strategy and the process development will be discussed. In this presentation, the synthesis of the complex target molecule will encompass the greening of a chiral isoxazoline production, continuous flow chemistry of a critical heteroaryl bromide-metal exchange and telescoped heteroaryl anion addition, and the GMP endgame development in multiple clinical campaigns.
Bryan Li is currently a Research Fellow in the Chemical R & D of Pharmaceutical Science Small Molecule division, Pfizer Inc., Groton, Connecticut, USA. He received his B.Sc. from Eastern University of Science & Technology, Shanghai, China in 1986, and Ph.D. in 1993 from University of Rhode Island, USA under the guidance of Prof. Elie Abushanab. Subsequently, he worked in Prof. Gary Posner’s group at the Johns Hopkins University at Baltimore, Maryland as a postdoctoral fellow for two years. In 1998, he joined Pfizer as a process chemist, and serves as a program lead responsible for exploratory development of drug candidates. In addition, Dr. Li has been leading and driving the development and implementation of continuous flow processes in the production in Pfizer.