新产品编号:2087167

Chemical Name: N1-[3-(N-Benzyloxysulfamoyl)-1(S)-(2-phenylethyl)-2-propenyl]-N2-(morpholin-4-ylcarbonyl)-L-phenylalaninamide
项目整合开发状态: Biological Testing
项目研究机构: University of California, San Francisco (Originator), University of Michigan (Originator)
合成路线:The Horner-Wadsworth-Emmons olefination of N-(tert-butoxycarbonyl)-L-homophenylalaninal (I) with phosphonate (II) by means of NaH in THF gives the vinylsulfonate (III),which is treated with tetrabutylammonium iodide and triphosgene to yield the sulfonyl chloride (IV).The reaction of (IV) with O-benzylhydroxylamine in dichloromethane affords the N-sulfonylhydroxylamine derivative (V),which is deprotected with TFA in dichloromethane,providing compound (VI) with a free amino group.Finally,this compound is condensed with N-(morpholin-4-ylcarbonyl)-L-phenylalanine (VII) by means of HOBt,EDC and NMM in DMF,giving rise to the target amide.