Non-adherence is a major hurdle for the effective treatment and prevention 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 subnanomolar antiviral activity and a long intracellular half-life. To support this program, we turned to biocatalysis to achieve a world-class manufacturing route from two simple building blocks, 2-ethynylpropane-1,2,3-triol and 2-fluoroadenine. This presentation will detail the innovations made in synthetic chemistry, biocatalysis, and process chemistry in route to a commercial manufacturing route for MK-8591.

Development of two simple building blocks for the biocatalytic synthesis of MK-8591

2019 Fall National Meeting

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