TSU-68, SU-6668

5-[(1,2-二氢-2-氧代-3H-吲哚-3-基)甲基]-2,4-二甲基-1H-吡咯-3-丙酸Chemical Name: (Z)-3-[2,4-Dimethyl-5-(2-oxo-2,3-dihydro-1H-indol-3-ylidenemethyl)-1H-pyrrol-3-yl]propionic acid
CAS No. 252916-29-3
项目整合开发状态: Phase II
项目研究机构: Sugen (Originator), Taiho (Licensee), Cancer Research UK (Codevelopment)
合成路线:Basic hydrolysis of the known 2,4-dimethyl-5-ethoxycarbonyl-3-(2-ethoxycarbonyl ethyl)pyrrole (I) and subsequent decarboxylation of the resulting diacid (II) in the presence of HCl furnished 2,4-dimethyl-3-pyrrolepropionic acid (III).Vilsmeier formylation of (III) employing dimethylformamide and POCl3 produced aldehyde (IV).The title compound was then obtained by condensation of aldehyde (IV) with oxindole (V) in the presence of pyrrolidine,followed by acid treatment of the intermediate (VI).Alternatively,direct condensation of aldehyde (IV) with oxindole (V) in the presence of NaOH gave rise to the title compound.