新产品编号:2457355

Chemical Name: 2-Cyano-2-[5-fluoro-1-(4-methylbenzyl)-2-oxo-2,3-dihydro-1H-indol-3-yl]acetic acid
项目整合开发状态: Preclinical
项目研究机构: Farmigea (Originator)
合成路线:5-Fluoroisatin (I) is alkylated with 4-methylbenzyl bromide (II) in the presence of NaH to afford the N-benzyl isatin derivative (III).Then,Knoevenagel condensation of isatin (III) with cyanoacetic acid (IV) by means of triethylamine in dioxane gives the indolinylidene adduct (V) as a mixture of E and Z isomers.Subsequent catalytic hydrogenation of (V) over Pd/C then furnishes the target compound

合成路线:5-Fluoroisatin (I) is alkylated with 4-methylbenzyl bromide (II) in the presence of NaH to afford the N-benzyl isatin derivative (III).Then,Knoevenagel condensation of isatin (III) with isopropyl cyanoacetate (IV) by means of piperidine in isopropanol gives the indolinylidene adduct (V) as a mixture of E and Z isomers.Subsequent catalytic hydrogenation of (V) over Pd/C then furnishes the target compound