新产品编号:650711

Chemical Name: N2-[N-(Benzyloxycarbonyl)-L-histidyl]-N1-(2-methyl-2-phenylpropyl)-N2-[1(R)-phenylethyl]glycinamide
CAS No. 248603-60-3
项目整合开发状态: Biological Testing
项目研究机构: Pfizer (Originator)
合成路线:The alkylation of (R)-alpha-methylbenzylamine (I) with methyl bromoacetate (II) gave aminoacetate (III).This was coupled with protected histidine (IV) by means of HATU as the coupling agent,yielding the protected dipeptide (V).Subsequent saponification of (V) using LiOH gave acid (VI).beta,beta-Dimethyl-phenethylamine (IX) was prepared by alkylation of phenylacetonitrile (VII) with iodomethane and NaH,followed by hydrogenation of the resulting dimethylated compound (VIII) in the presence of Raney Nickel.Coupling of amine (IX) with dipeptide (VI) provided the corresponding amide (X).The trityl protecting group of (X) was finally removed by treatment with trifluoroacetic acid.