新产品编号:1190173

Chemical Name: N1,N1'-[3(R),4(R)-Dihydroxy-1,6-diphenylhexane-2(S),5(S)-diyl]bis(benzyloxycarbonyl-L-alanyl-L-valinamide)
项目整合开发状态: Preclinical
项目研究机构: Scripps Clinic (Originator)
合成路线:Diol (I) was protected as the isopropylidene ketal (III) by reaction with 2,2-dimethoxypropane (II) and p-toluenesulfonic acid.Then,the N-carbobenzoxy groups of (III) were eliminated by hydrogenolysis on Pd/C to give the diamine (IV),and this was coupled with N-carbobenzoxy-valine (V) using O-benzotriazol-1-yl-tetramethyluronium hexafluorophosphate (HBTU) to afford (VI).A new sequence of hydrogenolytic Cbz deprotection to give diamine (VII) and coupling with N-carbobenzoxy-alanine (VIII) and HBTU provided (IX).Finally,the target compound was obtained by hydrolysis of the isopropylidene ketal in methanol containing p-toluenesulfonic acid.