PROCESS FOR THE PREPARATION OF AN INHIBITOR OF PHOSPHODIESTERASE 4

PROCESS FOR THE PREPARATION OF AN INHIBITOR OF PHOSPHODIESTERASE 4

The present invention relates to a process for the preparation of Crisaborole in a particular crystalline form 1 as an inhibitor of phosphodiesterase 4, in particular of phosphodiesterase 4B (PDE4B), and intermediates useful for its preparation. The claimed process is characterized by preparing the...

Ausführliche Beschreibung

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Bibliographische Detailangaben
Hauptverfasser: Razzetti, Gabriele, Lombardo, Alessandro, Vladiskovic, Chiara, Attolino, Emanuele, Santillo, Niccolò, Brenna, Davide
Format: Patent
Sprache:hrv ; eng
Schlagworte:
ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM
CHEMISTRY
METALLURGY
ORGANIC CHEMISTRY
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Beschreibung
Zusammenfassung:The present invention relates to a process for the preparation of Crisaborole in a particular crystalline form 1 as an inhibitor of phosphodiesterase 4, in particular of phosphodiesterase 4B (PDE4B), and intermediates useful for its preparation. The claimed process is characterized by preparing the Crisaborole by hydrolysis of the C-C-alkyl ester of formula (X):The crystalline Form 1 is characterized by an XRPD spectrum wherein the most intense peaks, measured using Cu Kα radiation (λ = 1.54 Å), fall at 6.0, 12.1, 14.1, and 15.4 ± 0.2° in 2θ.