新产品编号:1465441

Chemical Name: 2-(3',5'-Diethoxy-2-fluorobiphenyl-4-yl)propionic acid
项目整合开发状态: Biological Testing
项目研究机构: Merck Frosst (Originator)
合成路线:The acylation of 3,5-diethoxyphenol (I) with triflic anhydride gives the corresponding triflate (II),which is condensed with 2-(4-bromophenyl)propionic acid methyl ester (III) by means of triphenylphosphine and Pd2(dba)3 yielding 2-(3',5'-diethoxybiphenyl-4-yl)propionic acid methyl ester (IV).Finally,this compound is hydrolyzed with NaOH in methanol/water.

合成路线:The acylation of 3,5-diethoxyphenol (I) with triflic anhydride gives the corresponding triflate (II),which is condensed with 2-(4-bromo-3-fluorophenyl)propionic acid methyl ester (III) by means of triphenylphosphine and Pd2(dba)3 yielding 2-(3',5'-diethoxy-2-fluorobiphenyl-4-yl)propionic acid methyl ester (IV).Finally,this compound is hydrolyzed with NaOH in methanol/water.

合成路线:The cyclization of 4-iodoaniline (I) with 1-(phenylsulfanyl)acetone (II) by means of tert-butyl hypochlorite in dichloromethane gives the iodoindole (III),which is condensed with the phenylboronic ester (IV) using a Pd catalyst in DMSO to yield 2-[4-[2-methyl-3-(phenylsulfanyl)-1H-indol-5-yl]phenyl]propionic acid methyl ester (V).The desulfurization of (V) with thiosalicylic acid in hot TFA affords 2-[4-(2-methyl-1H-indol-5-yl)phenyl]propionic acid methyl ester (VI),which is finally hydrolyzed with LiOH in THF/methanol/water.