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Synfacts 2021; 17(05): 0479
DOI: 10.1055/s-0040-1719790
DOI: 10.1055/s-0040-1719790
Synthesis of Natural Products and Potential Drugs
Synthesis of Delgocitinib
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.
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.
Key words
delgocitinib - Janus kinase inhibitor - diastereoselective enolate alkylation - spirocyclization - β-lactam ring formation
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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Publication History
Article published online:
20 April 2021
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