新产品编号:2284917
Chemical Name: 2'-Deoxy-3'-O-[4-[2-(2-hydroxyethoxy)ethoxy]-4-oxobutyryl]-5-iodouridine
项目整合开发状态: Preclinical
项目研究机构: Universit?degli Studi di Catania (Originator), Universit?degli Studi di Perugia (Originator), Universit?degli Studi di Sassari (Originator), Universit?di Napoli Federico II (Originator)
合成路线:5-Iodo-2'-deoxyuridine (I) is protected at the primary hydroxyl group with 4,4'-dimethoxytrityl chloride to afford the 5'-O-trityl derivative (II).Subsequent esterification of the remaining hydroxyl group of (II) with succinic anhydride (III) yields the succinate mono-ester (IV).Acid (IV) is then coupled with diethylene glycol in the presence of DCC to produce (V).The O-trityl group of (V) is finally removed by treatment with formic acid,to give the title compound.
合成路线:5-Iodo-2'-deoxyuridine (I) is protected at the primary hydroxyl group with 4,4'-dimethoxytrityl chloride to afford the 5'-O-trityl derivative (II).Subsequent esterification of the remaining hydroxyl group of (II) with succinic anhydride (III) yields the succinate mono-ester (IV).Acid (IV) is then coupled with triethylene glycol in the presence of DCC to produce (V).The O-trityl group of (V) is finally removed by treatment with formic acid,to give the title compound.
📌 参考资料/链接:
参考文献标题:New oligoethylene ester derivatives of 5-iodo-2'-deoxyuridine as dermal prodrugs: Synthesis,physicochemical properties,and skin permeation studies
文献作者:Bonina,F.P.; Rimoli,M.G.; Avallone,L.; Barbato,F.; Amato,M.; Puglia,C.; Ricci,M.; De Caprariis,P.
参考来源:J Pharm Sci 2002,91(1),171