130707-89-0Relevant academic research and scientific papers
Unexpected Selectivity in the Alkylation of Polyazamacrocycles
Kruper, William J.,Rudolf, Philip R.,Langhoff, Charles A.
, p. 3869 - 3876 (1993)
Reaction of equivalent amounts of free base polyazamacrocycles with an alkyl halide in a nonpolar, aprotic solvent affords the mono-N-alkylation product as its monohydrohalide salt in high yield with excellent selectivity.This unexpected selectivity has been explained in terms of the high affinity of the alkylated product for a single proton which attenuates the nucleophilicity of the remaining nitrogen atoms.Selectivity is dependent upon a number of factors including macrocycle ring size, solvent polarity, and the steric nature of the electrophile.The approach has been allowed for a short, convergent route to bifunctional lanthanide chelators which are useful in therapeutic applications.
Macrocyclic tetraazacyclododecane conjugates and their use as diagnostic and therapeutic agents
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, (2008/06/13)
A group conjugates having a functionalized polyaminocarboxylate chelant that form complexes with rare earth-type metal ions, covalently attached to an antibody or antibody fragment, can be used for therapeutic and/or diagnostic purposes.
