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US 2019/0241585 A1Published application
Intermediates and process for the preparation of a crystalline form of a topical anti-inflammatory agent
AssigneeDipharma Francis S.R.L.
InventorsNiccolo' Santillo, Emanuele Attolino, Davide Brenna, Chiara Vladiskovic, Alessandro Lombardo, Gabriele Razzetti
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Abstract
The present invention relates to a process for the preparation of an inhibitor of phosphodiesterase 4, in particular of phosphodiesterase 4B (PDE4B), and intermediates useful for its preparation.
Claims16
A process for preparing Crisaborole in crystalline form 1 having an XRPD spectrum comprising peaks falling at 6.0, 12.1, 14.1, and 15.4±0.2° in 2θ, said process comprising:
- i) hydrolizing Crisaborole C1-C5 alkyl ester of formula (X)
- wherein R1 is a C1-C5 alkyl group.
Crisaborole C1-C5 alkyl ester of formula (X)
- wherein R1 is a C1-C5 alkyl.
Dependencies are inferred from the claim text.