N-1-CARBOXYALKYL DERIVATIVES OF LSD

摘要

Novel derivatives of LSD having formula (I) wherein R1 is an alkyl, cycloalk yl or aryl group having 1 to 10 carbon atoms, preferably an alkyl group having 1 carbon atom; R2 is a bond or (a) wherein R3 is an alkyl, cycloalkyl or aryl group h aving 2 to 10 carbon atoms, preferably an alkyl group having 2 or 5 carbon atoms; Z is an immunogenic carrier substance, an enzyme donor polypeptide or a label select ed from the group consisting of an enzyme, a substance having fluorescent or luminescent properties and a radioactive substance; and n is 1 to p where p equals MW of Z/1000. Th e derivatives include maleimide conjugates of an immunogenic poly(amino acid), an enzyme d onorpolypeptide or a labeling substance such as an enzym e, a fluorescent substance or a radioactive substance. Novel activated hapten intermediates useful in the p reparation of the conjugates and method for synthesis of the hapten intermediates and thei r conjugate derivatives are also disclosed.