SQ-094
Chemical Name: 4-[6-(4,6-Diphenyl-2-pyridinyloxy)-2,2-dimethylhexylamino]-4-oxo-3-(3-pyridinylcarboxamido)butanoic acid
CAS No. 206263-67-4 ([(S)-isomer])
项目整合开发状态: Biological Testing
项目研究机构: Bristol-Myers Squibb (Originator)
合成路线:The reduction of 6-(4,6-diphenylpyridin-2-yloxy)-2,2-dimethylhexanenitrile (I) (J Med Chem 1992,35: 4315) with NaBH4/TFA in THF gives 6-(4,6-diphenylpyridin-2-yloxy)-2,2-dimethylhexylamine (II),which is condensed with protected aspartic acid activated as succinimidyl ester (III) and triethylamine in DMF yielding te proteted aspartic acid amide (IV).The deprotection of (IV) with trifluoroacetic acid affords unprotected aspartamide (V),which is finally condensed with pyridine-3-carboxylic acid succinimidyl ester (VI) by means of triethylamine in DMF.
📌 参考资料/链接:
参考文献标题:Radiopharmaceuticals for imaging infection and inflammation
文献作者:Rajopadhye,M.; Harris,T.D.; Barrett,J.A.; Cheesman,E.H.(DuPont Pharmaceuticals Co.)
参考来源:WO 9815295