Process for the preparation of imidazoleacetic acid derivatives

Claim 1

A process for preparing an imidazoleacetic acid derivative of the formula ##STR7## wherein R 1 is hydrogen; C 1-24 -alkyl; C 5-7 -cycloalkyl; C 7-14 -aralkyl; C 6-14 -aryl; a C 6-10 -aromatic, mono- or bi-cyclic heterocycle of 5-10 total ring atoms, 1-3 being O, N or S atoms, the remainder being C-atoms; substituted C 6-14 -aryl or said aromatic heterocycle each substituted by 1-3 halogen atoms, up to three C 1-4 -alkyl groups, a nitro group, up to three C 1-4 -alkoxy groups, a C 1-4 -alkoxycarbonyl group or CF 3 ; amino; or amino substituted by C 1-24 -alkyl, C 5-7 cycloalkyl, C 7-14 -aralkyl or C 6-14 aryl; R 2 , independently, is hydrogen, alkyl, cycloalkyl, aralkyl, aryl, or a heterocyclic group, all as defined above for R 1 ; or R 1 and R 2 together are C 4-7 alkylene forming a ring with their connecting C-N bond; and R 3 is C 1-10 -alkoxy, C 7-14 -aralkoxy, amino, mono or di-C 1-4 -alkylamino, pyrrolidino, piperidino, morpholino, arylamino, heteroarylamino, or substituted arylamino or substituted heteroarylamino, each of which is substituted in the aryl portion as recited above for R 1 ; comprising reacting a corresponding amidine or guanidine of the formula ##STR8## or a reaction compatible acid addition salt thereof wherein R 1 and R 2 are as defined above with an acetoacetic acid derivative of the formula ##STR9## wherein R 3 is as defined above and X is fluorine, chlorine, bromine, or iodine, and R 4 is tri-C 1-4 -alkyl or tri-C 7-10 -aralkylsilyl, C 1-4 -alkyl, or C 7-10 -aralkyl