K-777, CRA-3316, APC-3316, K-11777

Chemical Name: N-(4-Methylpiperazin-1-ylcarbonyl)-L-phenylalanine 1(S)-(2-phenylethyl)-3-(phenylsulfonyl) -2(E)-propenyl amide
CAS No. 233277-99-1
项目整合开发状态: Preclinical
项目研究机构: Celera (Originator), Institute for OneWorld Health (Licensee), National Institutes of Health (Codevelopment)
合成路线:Phosphonylation of the lithium anion of phenyl methyl sulfone (I) with diethyl chlorophosphate afforded the sulfonyl phosphonate (II).This was condensed with N-Boc-L-homophenylalaninal (III) under Wadsworth-Emmons conditions to furnish the vinyl sulfone (IV).After acidic Boc group cleavage,the resultant amine (V) was coupled with the N-carbamoyl phenylalanine (VI),via the corresponding mixed anhydride with isobutyl chloroformate,to afford the target amide.