PROCESS FOR THE PREPARATION OF PYRAZOLOPYRIDINE DERIVATIVES

摘要

The invention provides a process for preparing a compound of formula (I) and pharmaceutically acceptable derivatives thereof wherein: R and R<1> are independently selected from H, halogen, C1-6alkyl, C1-6alkoxy, or C1-6alkoxy substituted by one or more fluorine atoms; R<2> 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<4>R<5>, CO2H, CO2C1-6alkyl, or NHSO2R<4>; R<3> is H or phenyl substituted by SO2C1-6alkyl or SO2NH2; R<4> and R<5> are independently selected from H, C1-6alkyl, phenyl, phenyl substituted by one or more atoms or groups R<6>, or together with the nitrogen atom to which they are attached form a saturated 4 to 8 membered ring R<6> 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<0> to R<3> are as defined for formula (I), or a protected derivative thereof, in the presence of a catalyst and a solvent.