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Synthesis and radiolabeling of a biotin‐CHX‐B chelate for Bi‐213
Author(s) -
Pathare P. M.,
Hamlin D. K.,
Wilbur D.S.,
Brechbiel M. W.,
Bray L. A.
Publication year - 1998
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/(sici)1099-1344(199807)41:7<595::aid-jlcr116>3.0.co;2-o
Subject(s) - chemistry , biotin , yield (engineering) , chelation , derivative (finance) , chemical synthesis , combinatorial chemistry , radiochemistry , stereochemistry , nuclear chemistry , organic chemistry , biochemistry , in vitro , materials science , economics , financial economics , metallurgy
The synthesis and radiolabeling of a biotin derivative which contains a chelating group (CHX‐B) for binding the α‐emitting radionuclide, 213 Bi, is described. The biotin‐CHX‐B derivative was readily prepared in high yield through a convergent synthesis that coupled N‐methylglycylbiotinamide with anilino‐CHX‐B. Bismuth‐213 labeling of the biotin‐CHX‐B molecule was facile at room temperature, resulting in >95% radiochemical yield within 10 min reaction time. © 1998 John Wiley & Sons, Ltd.