4.6 Article

Development of a Nitrene-Type Rearrangement for the Commercial Route of the JAK1 Inhibitor Abrocitinib

Journal

ORGANIC PROCESS RESEARCH & DEVELOPMENT
Volume 25, Issue 3, Pages 608-615

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.oprd.0c00366

Keywords

process chemistry; Curtius rearrangement; Lossen rearrangement; biocatalysis; JAK inhibitor; Pfizer

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The development of a commercial route towards the JAK1 inhibitor abrocitinib involves a late-stage Lossen rearrangement to obtain the desired compound, which is then sulfonylated using a novel water-tolerable triazole sulfonylating reagent to provide the active pharmaceutical ingredient.
The development of a commercial route toward the JAK1 inhibitor abrocitinib is described. The application of a late-stage Lossen rearrangement provided the desired cis-diaminocyclobutane, which was subsequently sulfonylated using a novel water-tolerable triazole sulfonylating reagent to provide the active pharmaceutical ingredient.

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