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oai:figshare.com:article/34032154 2026-09-30T12:11:30Z category_1 category_4 category_7 category_13 category_15 category_19 category_272 category_734 category_61 category_62 category_132 portal_63 item_type_6 month_year_09_2026

Synthetic Development and Scale-Up of the Aminoindazole Fragment of Lenacapavir Lennie Lin (10751217) Anna M. Wagner (1837234) Jason Davy (25143805) Chloe Y. Wong (25143808) Wen-Tau T. Chang (2389168) B. Michael O’Keefe (1530931) Alexander F. G. Goldberg (9630041) Huy Van Huynh (25143811) Hongwei Sun (422270) Wei Wang (17594) Scott A. Wolckenhauer (2283733) Biophysics Biochemistry Medicine Genetics Neuroscience Pharmacology Environmental Sciences not elsewhere classified Biological Sciences not elsewhere classified Developmental Biology Marine Biology Infectious Diseases purpose ” large mediated nitrile formation key improvements include initial “ fit final product quality drug recently approved >- sulfonic acid commercially viable process development efforts improved 1 </ b yielding process process safety yeytuo ). synthetic development step route significant overhaul hydroxylamine -< exposure prophylaxis describe herein alternative condition acting treatment We describe herein the development and scale-up of the aminoindazole fragment of lenacapavir, a drug recently approved for long-acting treatment of HIV (Sunlenca) and pre-exposure prophylaxis (as Yeztugo and Yeytuo). This five-step route to fragment <b>1</b> was developed from the initial “fit-for-purpose” large-scale synthesis to a commercially viable process. Key improvements include an alternative condition to hydroxylamine-<i>O</i>-sulfonic acid-mediated nitrile formation and a significant overhaul of the key Miyaura borylation process. The culmination of all development efforts improved the final product quality and process safety, resulting in a more efficient and higher-yielding process. 2026-09-30T00:00:00Z Text Journal contribution 10.1021/acs.oprd.6c00302.s001 https://figshare.com/articles/journal_contribution/Synthetic_Development_and_Scale-Up_of_the_Aminoindazole_Fragment_of_Lenacapavir/34032154 CC BY-NC 4.0