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Organic Chemistry - Merck Symposium

Wednesday, June 12, 2019
3:30pm to 5:00pm
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Noyes 153 (J. Holmes Sturdivant Lecture Hall)
Novel Catalytic Approaches to the Synthesis of a Complex Drug Molecule
Dr. Aaron Whittaker, Associate Principal Scientist, Department of Process Research and Development, Merck & Co. Inc.,

Non-adherence is a major hurdle for the effective treatment of HIV, a global epidemic even after 30 years of medical advancements. Long-acting therapeutics have the potential to improve adherence through simplified regimens. One such investigational medication is MK-8591, a nucleoside reverse transcriptase translocation inhibitor with sub-nanomolar antiviral activity and a long intracellular half-life. To support this program, a world-class manufacturing synthesis which is robust, green, and sustainable was targeted. In this presentation, I will describe how our team has addressed the long standing challenge of stereoselective glycosylation with a novel four-enzyme biocatalytic cascade. I will also discuss various routes developed to efficiently complete the synthesis, and the catalytic methods developed to enabled each approach. Highlights include two new methods for enantioselective ketone alkynylation, and a route consisting of nine enzymes carried through one pot.

For more information, please contact Annette Luymes by phone at 626-395-6016 or by email at [email protected].