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Synthesis of Delgocitinib
Stereocontrolled Synthesis of Delgocitinib, a JAK Inhibitor for the Treatment of Atopic Dermatitis.
Org. Process Res. Dev. 2021;
Key wordsdelgocitinib - Janus kinase inhibitor - diastereoselective enolate alkylation - spirocyclization - β-lactam ring formation
Delgocitinib is a Janus kinase inhibitor that has been approved in Japan for the treatment of atopic dermatitis. The FDA has granted Fast Track Designation to delgocitinib cream for the treatment of adult moderate-to-severe chronic hand eczema.
The route to delgocitinib depicted delivered the API in 39% overall yield in nine steps without recourse to cryogenic conditions or chromatographic purification. This route has been implemented on a 60 kg scale.
20 April 2021 (online)
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