PIPERIDINE ANALOGS AND CONJUGATES OF PROCAINAMIDE AND NAPA

摘要

Novel derivatives of procainamide and N-acetylprocainamide (NAPA) are disclosed having formula (1) wherein: X = hydrogen or acetyl; n = 1 to p where p = MW of Z/1000; Z = a poly(amino acid) or polysaccharide; and R3 = a bond or (2) wherein R2 = an alkyl, cycloalkyl or aryl group having 2 to 10 carbon atoms. The derivatives include maleimide conjugates of proteins or poly(amino acids), enzymes, enzyme donor polypeptides and labeling substances. Novel activated conjugates and methods for synthesis of the hapten intermediates and derivatives are also disclosed.