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
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.
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.
