Pl. Anelli et al., DOTA tris(phenylmethyl) ester: A new useful synthon for the synthesis of DOTA monoamides containing acid-labile bonds, BIOCONJ CHE, 12(6), 2001, pp. 1081-1084
The synthesis of DOTA tris(phenylmethyl) ester 2, a new monoreactive deriva
tive of DOTA, is described. This versatile synthon can be easily coupled to
compounds bearing an amino group and then deprotected to DOTA monoamide un
der mild and neutral conditions by catalytic hydrogenolysis. Accordingly, c
ompound 2 has been used in the synthesis of a DOTA monoamide gadolinium com
plex containing two palmitic esters, which is a component of mixed micelles
as MRI contrast agents.