Patent ID: 6046340
Filing Date: 2000-04-04
Classification: A61K,A61P,A61Q,C07D,C12P

Abstract:
Chemical process for the preparation of the product of the formula: ##STR23## in which A is:a) ##STR24## in which B is primary amine; secondary amine of the formula --NH--X in which X is hydrocarbon, fluoroalkyl, acyl or amine; cycloalkyl or lactam tertiary cyclic amine; --N(--Y)--Y' in which Y and Y' are hydrocarbon, acyl or acyloxy; --N.dbd.C(--Y)--Y' in which Y is hydrocarbon and Y' is hydrogen or hydrocarbon; or ##STR25## in which Y, Y' and Y"" are hydrocarbon and the counter ion W is halide, sulfate, phosphate, bicarbonate, para-toluene sulfonate or a carboxylic acid-containing radical,R is fluorine, fluoroalkyl, a functional group selected from the group consisting of sulfate, phosphate and carboxylic acid, acyl, linear C.sub.2-6 alkyl unsubstituted or substituted by one or more said functional groups, alkenyl or aryl optionally substituted by one or more said functional groups, andR' is hydrogen, fluorine, alkyl or fluoroalkyl; orb) ##STR26## in which R is hydrogen, fluorine, fluoroalkyl, acyl or hydrocarbon unsubstituted or substituted by one or more said functional groups and R"" is acyl or hydrocarbon optionally substituted by one or more said functional groups, andIm is an imidazole or N-substituted imidazole comprising the following steps:N-protecting said alpha aminoacid by a group X,O-activating said alpha aminoacid by a group Y,Coupling said N-protected and O-activated alpha amino acid with histamine or methyl-substituted histamine.