PROCESS FOR THE PREPARATION OF PYRAZOLOPYRIDINE DERIVATIVES

The invention provides a process for preparing a compound of formula (I) and pharmaceutically acceptable derivatives thereof wherein: R and R are independently selected from H, halogen, C1-6alkyl, C1-6alkoxy, or C1-6alkoxy substituted by one or more fluorine atoms; R is H, C1-6alkyl, C1-6alkyl subst...

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Bibliographische Detailangaben
Hauptverfasser:	JUNG, DAVID KENDALL, EADDY, JOHN F, FITZGERALD, RUSS N
Format:	Patent
Sprache:	eng ; fre ; ger
Schlagworte:	CHEMISTRY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Beschreibung
Zusammenfassung:	The invention provides a process for preparing a compound of formula (I) and pharmaceutically acceptable derivatives thereof wherein: R and R are independently selected from H, halogen, C1-6alkyl, C1-6alkoxy, or C1-6alkoxy substituted by one or more fluorine atoms; R is H, C1-6alkyl, C1-6alkyl substituted by one or more fluorine atoms, C1-6alkoxy, C1-6hydroxyalkyl, SC1-6alkyl, C(O)H, C(O)C1-6alkyl, C1-6alkylsulfonyl, C1-6alkoxy substituted by one or more fluorine atoms, halogen, CN, CONR R , CO2H, CO2C1-6alkyl, or NHSO2R ; R is H or phenyl substituted by SO2C1-6alkyl or SO2NH2; R and R are independently selected from H, C1-6alkyl, phenyl, phenyl substituted by one or more atoms or groups R , or together with the nitrogen atom to which they are attached form a saturated 4 to 8 membered ring R is halogen, C1-6alkyl, C1-6alkoxy or C1-6alkoxy substituted by one or more fluorine atoms; which comprises rearrangement of an azirine of formula (II) wherein R to R are as defined for formula (I), or a protected derivative thereof, in the presence of a catalyst and a solvent.