Plenary Lecture
Niki Patel, Ph.D.
Associate Principal Scientist, Process Research & DevelopmentMerck Research LaboratoriesInnovative Strategies toward Complex Molecule Synthesis: Development of a Fully Biocatalytic Manufacturing Route for Islatravir
A staggering 37 million people are currently living with HIV worldwide, with more than 2 million individuals newly infected every year. There is, therefore, an urgent need for a simplified treatment for this highly infectious disease to improve the overall quality of patient lives. Islatravir, a nucleoside reverse transcriptase translocation inhibitor (NRTTI) is a uniquely suited compound due to its high efficacy and potency, which has the potential to improve the overall quality of life for patients. On the road to developing a highly sustainable and green commercial manufacturing route, the process chemistry team has employed biocatalysis to facilitate the synthesis of this nucleoside. In a novel transformation, an enzymatic cascade sequence is utilized for the preparation of the 4’-ethynyl-2’-deoxyribose sugar fragment of the molecule. In addition, a highly selective glycosylation reaction involving another enzymatic system is used to fuse the 2-fluoroadenine base to the sugar component. This talk will focus on the progress surrounding the development of this unparalleled manufacturing route.