Patent ID: 7005520

Claim:
A process for the production of a compound of formula I: wherein A represents CH or N; R 1 represents H, lower alkyl (which alkyl group is optionally interrupted by O), Het, alkylHet, aryl or alkylaryl, which latter five groups are all optionally substituted (and/or, in the case of lower alkyl, optionally terminated) by one or more substituents selected from halo, cyano, nitro, lower alkyl, OR 5 , C(O)R 6 , C(O)OR 7 , C(O)NR 8 R 9 , NR 10a R 10b and SO 2 NR 11a R 11b ; R 2 and R 4 independently represent lower alkyl; R 3 represents lower alkyl, which alkyl group is optionally interrupted by oxygen; Het represents an optionally substituted four- to twelve-membered heterocyclic group, which group contains one or more heteroatoms selected from nitrogen, oxygen and sulfur; R 5 , R 6 , R 7 , R 8 , R 9 , R 11a and R 11b independently represent H or lower alkyl; R 10a and R 10b either independently represent, H or lower alkyl or, together with the nitrogen atom to which they are attached, represent azetidinyl, pyrollidinyl or piperidinyl, which process comprises the reaction of a compound of formula II, wherein R x is a groups substitutable by an aminopyrazole, selected from: —OR e , wherein R e independently represents the same groups as defined by R 1 ; —N H 2 ; —NHR a , wherein R a represents —OR 1 or halo; —N(R b )R c , wherein R b and R c each independently represent the same groups as defined by R 1 ; —SH; and —SR d ; wherein R d independently represents the same groups as defined by R 1 ; and A, R 3 and R 4 are as defined above, with a compound of formula III, wherein R 1 and R 2 are as defined above and wherein the compound of formula II is prepared by way of reaction of a compound of formula IV, wherein G represents a carboxylic acid group (—C(O)OH), CO 2 Et, —CN, —C(OR e ) 3 , —C(O)NH 2 , —C(═NOR f )N(R e ) 2 , wherein R f represents H or lower alkyl and R e is as hereinbefore defined, 5- or 6-membered heterocyclic group containing at least two heteroatoms selected from O, S, N and mixtures thereof wherein the heterocyclic group is bonded by a carbon atom wherein the group G is converted to a —C(R x )═NH group.