Synfacts 2021; 17(05): 0479
DOI: 10.1055/s-0040-1719790
Synthesis of Natural Products and Potential Drugs

Synthesis of Delgocitinib

Rezensent(en):
Philip Kocienski
Takiguchi H, *, Higashi A, Watanabe T, Takeichi T, Shimazaki T, Inaba T. * Japan Tobacco Inc., Osaka, Japan
Stereocontrolled Synthesis of Delgocitinib, a JAK Inhibitor for the Treatment of Atopic Dermatitis.

Org. Process Res. Dev. 2021;
25: 342-348
DOI: 10.1021/acs.oprd.1c00031.
 

Significance

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.


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Comment

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.


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Publikationsverlauf

Publikationsdatum:
20. April 2021 (online)

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