Method for preparing bicyclic compounds and use of said...

Details Method for preparing bicyclic compounds and use of said... Method for preparing bicyclic compounds and use of said...

C - Chemistry, Metallurgy

07

K

C07K 5/078 (2006.01) C07D 237/04 (2006.01)

Patent

CA 2359964

The invention concerns a method for preparing compounds of formula (I) wherein: R = H, alkyl, aryl, aralkyl containing up to 18 carbon atoms and the amine function may be free or protected, from a compound of formula (IA). The invention is characterised in that the cyclization is carried out in a basic medium and in the presence of a phosphonic acid derivative in particular POCl¿3? or POBr¿3?. The invention also concerns the use of said method as an intermediate step for preparing a compound inhibiting the interleukin-1 beta conversion enzyme (ICE).

L'invention a pour objet un procédé de préparation des composés de formule (I) dans laquelle R = H, alkyle, aryle ou aralkyle renfermant jusqu'à 18 atomes de carbone et la fonction amine peut être libre ou protégée, à partir d'un composé de formule (IA) caractérisé en ce que la cyclisation s'effectue en milieu basique et en présence d'un dérivé d'acide phosphonique notamment POCl3 ou POBr3 et l'application de ce procédé comme étape intermédiaire pour la préparation d'un composé inhibiteur de l'enzyme de conversion de l'interleukine 1-bêta (ICE).

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