【药物名称】
化学结构式(Chemical Structure):
参考文献No.41524
标题:Functionalized alkyl and alkenyl side chain derivs. of glycinamides as farnesyl transferase inhibitors
作者:Doherty, A.M.; Quin, J. III; Kaltenbronn, J.S.; Leonard, D.M.; McNamara, D.J. (Pfizer Inc.)
来源:WO 9955725
合成路线图解说明:

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.

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