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  Lenacapavir Synthesis Highlights

  In this guest article, Dr. Luíza Cruz breaks down the synthesis of Gilead’s lenacapavir (GS-6207), Drug Hunter’s Small Molecule of the Year – 2020. Lenacapavir is a promising first-in-class, long-acting injectable (LAI) HIV capsid inhibitor. Interesting synthetic steps employed in this route include an unusual sodium chlorite-mediated benzylic oxidation, efficient installation of the gem-difluoro moiety,…

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  June 2022 Molecules of the Month Runners-Up

  Readers have been asking for more molecules, so we started a new feature that highlights a few of the molecules we liked that didn’t make it into Molecules of the Month. There were six runners-up this month, including an orally available ALK2 inhibitor and a direct AMPK activator for X-linked adrenoleukodystrophy. You can read more…

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  Literature Highlights from April and May 2022

  There’s so many interesting new publications that don’t necessarily feature key molecules, but are helpful for drug hunters to know about. Here are some other interesting reviews, technology, and targets to watch from April and May: April 2022 Best Practices: Understanding PK-PD for Protein Degraders: A Review. Derek Bartlett and Adam Gilbert from Pfizer have…

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  May 2022 Molecules of the Month Runners Up

  Readers have been asking for more molecules, so this month, we’re starting a new feature that will highlight a few of the molecules we liked that didn’t make it into Molecules of the Month. There were six runners-up this month, including an orally bioavailable, brain penetrant inhibitor of PAAN/MIF, and a STING agonist discovered using…

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  Small Molecule Long-Acting Injectables (LAIs) Leading to a Paradigm Shift in HIV Treatment and Prophylaxis

  In this highlight, Dr. Dennis C. Koester reviews treatment options for HIV and explains how small molecule long-acting injectables (LAIs) are offering significant promise in both HIV treatment and prophylaxis. A Coming Paradigm Shift for HIV Treatment and Prophylaxis By Dennis C. Koester The surge of the coronavirus pandemic has made our society increasingly aware…

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  Production-Scale Synthesis of gem-Dimethylcyclopropylproline

  The gem-dimethylcyclopropyl group is a key element in drugs, candidates, and agrochemicals, with a recent example being nirmatrelvir, the active ingredient in the Pfizer COVID-19 drug, Paxlovid. Here, we review synthetic strategies used to produce the key gem-dimethylcyclopropylproline intermediate, which may now be required in hundred-ton quantities to support nirmatrelvir manufacturing. Synthesis Spotlight: The gem-Dimethylcyclopropyl…