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- W4253200475 abstract "A novel and practical desymmetrization tactic is described to access a new class of pibrentasvir prodrugs. The homotopic benzimidazoles of pibrentasvir (PIB) are differentiated via a one-pot di-Boc/mono-de-Boc selective <i>N</i>-Boc protection and formaldehyde adduct formation sequence, both enabled by crystallization-induced selectivity. The first step represents the only known application of the Horeau principle of statistical amplification for <i>C</i><sub>2</sub>-symmetric polyheterocycle regioselective functionalization. The resulting versatile intermediate is employed in the high-yielding preparation of several pibrentasvir prodrug candidates." @default.
- W4253200475 created "2022-05-12" @default.
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- W4253200475 date "2021-04-28" @default.
- W4253200475 modified "2023-09-25" @default.
- W4253200475 title "Desymmetrization of Pibrentasvir for Efficient Prodrug Synthesis" @default.
- W4253200475 doi "https://doi.org/10.26434/chemrxiv.14456259" @default.
- W4253200475 hasPublicationYear "2021" @default.
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