DOTA tris(phenylmethyl) ester: A new useful synthon for the synthesis of DOTA monoamides containing acid-labile bonds
DOTA tris(phenylmethyl) ester: A new useful synthon for the synthesis of DOTA monoamides containing acid-labile bonds
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DOI：
10.1021/bc010046x
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发表时间：
2001-11-01
影响因子：
4.7
通讯作者：
Recanati, P
中科院分区：
文献类型：
--
作者：
Anelli, PL;Lattuada, L;Recanati, P
介绍了一种新的DOTA单活性衍生物——DOTA三苯基甲基酯2的合成。这种多功能的合成物可以很容易地偶联到含有氨基的化合物上，然后在温和和中性的条件下通过催化氢解脱保护成DOTA单酰胺。因此，化合物2已被用于合成含有两种棕榈酯的DOTA单酰胺钆配合物，该配合物是作为MRI造影剂的混合胶束组分。
The synthesis of DOTA tris(phenylmethyl) ester 2, a new monoreactive derivative of DOTA, is described. This versatile synthon can be easily coupled to compounds bearing an amino group and then deprotected to DOTA monoamide under mild and neutral conditions by catalytic hydrogenolysis. Accordingly, compound 2 has been used in the synthesis of a DOTA monoamide gadolinium complex containing two palmitic esters, which is a component of mixed micelles as MRI contrast agents.