KNI-1039
Chemical Name: 3'-Azido-5'-O-[2-[5-[1(S)-[4(R)-(N-tert-Butylcarbamoyl)-5,5-dimethylthiazolidin-3-ylcarbonyl]-2(S)-[2-(2,6-dimethylphenoxy)acetamido]-3-phenylpropoxy]-5-oxopentanamido]acetyl]-3'-deoxythymidine
项目整合开发状态: Biological Testing
项目研究机构: Kyoto Pharmaceutical University (Originator), Osaka Medical College (Originator)
合成路线:Coupling of AZT (I) with Boc-Gly-OH (II) by means of dicyclohexyl carbodiimide (DCC) in the presence of dimethylaminopyridine (DMAP) in DMF followed by Boc removal by treatment with HCl/dioxane yields AZT ester (III).On the other hand,KNI-727 (IV) is condensed with glutaric anhydride (V) in THF-ether in the presence of dicyclohexylamine (DCHA) to yield the half ester of KNI-727 (VI),which is then condensed with derivative (III) by means of EDC.HCl in DMF in the presence of HOBt to furnish the target compound.
📌 参考资料/链接:
参考文献标题:"Double-drugs" - a new class of prodrug form of an HIV protease inhibitor conjugated with a reverse transcriptase inhibitor by a spontaneously cleavable linker
文献作者:Matsumoto,H.; Hamawaki,T.; Ota,H.; Kimura,T.; Goto,T.; Sano,K.; Hayashi,Y.; Kiso,Y.
参考来源:Bioorg Med Chem Lett 2000,10(11),1227