| 摘要 |
A process and intermediates for the preparation of triazolopyrimidine compounds of formula I <CHEM> wherein R<1>, X, L<1>, L<2>, L<3>, L<4> and L<5> are as defined in the description, which comprises reacting alkyl 2-aryl-3-alkyl-3-oxopropionates of formula IV <CHEM> wherein R<1> and L<1>, L<2>, L<3>, L<4> and L<5> are as defined for formula I and R' represents an optionally substituted alkyl group, a) with 2-amino-Ä1,3,4Ü-triazole, and treating the resulting 5-hydroxytriazolopyrimidines of formula I, wherein X represents a hydroxy group, with a halogenating agent, and b) optionally treating the resulting 5-hydroxytriazolopyrimidines with an alcohol or a thioalkohol in the presence of a base, or with a metal amide, a metal alkyl amide or a metal dialkylamide, or a metal cyanide.A process and intermediates for the preparation of triazolopyrimidine compounds of formula I <CHEM> wherein R<1>, X, L<1>, L<2>, L<3>, L<4> and L<5> are as defined in the description, which comprises reacting alkyl 2-aryl-3-alkyl-3-oxopropionates of formula IV <CHEM> wherein R<1> and L<1>, L<2>, L<3>, L<4> and L<5> are as defined for formula I and R' represents an optionally substituted alkyl group, a) with 2-amino-Ä1,3,4Ü-triazole, and treating the resulting 5-hydroxytriazolopyrimidines of formula I, wherein X represents a hydroxy group, with a halogenating agent, and b) optionally treating the resulting 5-hydroxytriazolopyrimidines with an alcohol or a thioalkohol in the presence of a base, or with a metal amide, a metal alkyl amide or a metal dialkylamide, or a metal cyanide. |
