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新产品编号:1644207

Chemical Name: 6-(2-Acetoxyethyl)-3,12-bis(carboxymethyl)-9-[2-(butyryloxy)ethyl]-4,11-dioxo-3,6,9,12-tetraazatetradecane-1,14-dioic acid gadolinium complex
项目整合开发状态: Preclinical
项目研究机构: University of Alabama at Birmingham (Originator)
合成路线:The condensation of 2-bromo-N,N-bis(benzyloxycarbonylmethyl)acetamide (I) with N,N'-bis(2-hydroxyethyl)ethylene-1,2-diamine (II) by means of TEA in DMF gives the corresponding bis-adduct (III).The monoacylation of (III) with butyryl chloride (IV) and DMAP in THF yields the monobutyrate (V),which is acylated with acetyl chloride (VI) and DMAP in THF affording the mixed diester monoacetate monobutyrate (VII).The deprotection of (VII) by hydrogenation with H2 over Pd/C in ethanol provides the tetraacetic acid (VIII),which is finally treated with gadolinium trichloride and NaOH to furnish the target compound.
📌 参考资料/链接:
参考文献标题:Synthesis and in vivo evaluation of new contrast agents for cardiac MRI
文献作者:Saab-Ismail,N.H.; Simor,T.; Gaszner,B.; Lorand,T.; Szollosy,M.; Elgavish,G.A.
参考来源:J Med Chem 1999,42(15),2852