新产品编号:443469

Chemical Name: 2(S)-[5-[2-Cyclohexyl-1(S)-(ethylsulfanylmethyl)ethylaminomethyl]-2'-methylbiphenyl-2-ylcarboxamido]-4-(methylsulfanyl)butyric acid; N-[5-[2-Cyclohexyl-1(S)-(ethylsulfanylmethyl)ethylaminomethyl]-2'-methylbiphenyl-2-ylcarbonyl]-L-methionine
CAS No. 216230-06-7
项目整合开发状态: Preclinical
项目研究机构: University of Pittsburgh (Originator), Abbott (Codevelopment)
合成路线:Palladium-catalyzed coupling of dimethyl iodoterephthalate (I) with 2-methylphenylboronic acid (II) furnished the biphenyl derivative (III).Regioselective ester hydrolysis of (III) under controlled conditions provided the mono acid (IV),which was further reduced to alcohol (V) using borane in THF.After hydrolysis of the remaining ester function of (V),the resulting carboxylic acid (VI) was coupled to L-methionine methyl ester (VII),yielding amide (VIII).Swern oxidation of the alcohol function of (VIII) gave aldehyde (IX).This was then subjected to a reductive amination with amine (X) in the presence of NaBH(OAc)3 to afford the secondary amine (XI).The methyl ester group of (XI) was finally hydrolyzed with LiOH.