MALEIMIDE ADDUCT CONJUGATES OF PROCAINAMIDE AND NAPA

摘要

Novel derivatives of procainamide and N-acetylprocainamide (NAPA) are disclosed having formula (a) wherein: X = hydrogen or acetyl; R1 = an alkyl group having 1 to 3 carbon atoms; m = an integer from 2 to 10; R2 = an alkyl, cycloalkyl or aryl group having 2 to 10 carbon atoms; Z = a poly(amino acid); and n = 1 to p where p = MW of Z/1000. The derivatives include maleimide conjugates of proteins or poly(amino acids), enzymes, enzyme donor polypeptides and labelling substances. Novel activated hapten intermediates useful in the preparation of the conjugates and methods for synthesis of the hapten intermediates and derivatives are also disclosed.