DOTA tris(phenylmethyl) ester: A new useful synthon for the synthesis of DOTA monoamides containing acid-labile bonds

Citation
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
Citations number
26
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOCONJUGATE CHEMISTRY
ISSN journal
10431802 → ACNP
Volume
12
Issue
6
Year of publication
2001
Pages
1081 - 1084
Database
ISI
SICI code
1043-1802(200111/12)12:6<1081:DTEANU>2.0.ZU;2-9
Abstract
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.