新产品编号:1821391

Chemical Name: N-(2-Hydroxy-1,2-dioxoethyl)-4-(phosphonomethyl)-L-phenylalanyl-(1-aminocyclohexylcarbonyl)-L-asparagine 3-(5-methyl-1H-indol-1-yl)propylamide
项目整合开发状态: Biological Testing
项目研究机构: Georgetown University (Originator), National Cancer Institute (Originator)
合成路线:Coupling between asparagine amide (I) and N-Fmoc-1-amino-cyclohexanecarboxylic acid (II) afforded dipeptide amide (III).Deprotection of the Fmoc group of (III) to give (IV) was carried out by treatment with piperidine in DMF.Subsequent coupling of dipeptide (IV) with the protected phenylalanine derivative (V) using diisopropyl carbodiimide (DIC) and HOBt furnished tripeptide (VI),and further cleavage of the Fmoc group provided (VII).Acylation of (VII) with tert-butyl oxalyl chloride (VIII) yielded amide (IX).The tert-butyl ester groups of (IX) were finally cleaved by treatment with trifluoroacetic acid.