新型碘造影剂STL-05的合成

Synthesis of a new iodinated contrast agent STL-05

以3-氨基-5-(2,3-二乙酰氧基正丙胺基甲酰基)-2,4,6-三碘苯甲酸为原料,依次经氨基酰化、酰氯化、胺解和酯水解等4步反应得到标题化合物,结构经1HNMR和MS确证,其纯度≥98%(HPLC归一化法)。标题化合物理化性质优于碘海醇,值得进一步评价。

N-Methyl-N-（ 2-hydroxyethyl ）-N′-（ 2, 3-di- hydroxypropyl ） -5- （ 2-hydroxyaeetamido ） -2,4,6 -triiodoisoph- thalamide（ STL-05 ） was synthesized from 3-amino-5-（ 2,3-di- acetoxypropylcarbamoyl）-2,4,6-triiodobenzoic acid via ami- no-acylation, acyl chlorination, acylamination and esterolysis. STL-05（purity ≥98% ） was confirmed by 1^HNMR and MS. STL-05 has better physicochemical properties than iohexol and is worth further investigating.