新产品编号:2291245

Chemical Name: N5-(2-Carboxybenzoyl)-N2-[4-[2-(2,4-diaminoquinazolin-6-yl)ethyl]benzoyl]-L-ornithine
项目整合开发状态: Biological Testing
项目研究机构: Dana-Farber Cancer Institute (Originator), Harvard Medical School (Originator)
合成路线:Palladium-catalyzed coupling of 2,4-diamino-6-iodoquinazoline (I) with trimethylsilyl acetylene (II) affords the silylethynyl quinazoline (III).Subsequent treatment of (III) with tetrabutylammonium fluoride leads to the desilylated acetylene compound (IV).

合成路线:Condensation between phthaloyl ornithine methyl ester (V) and 4-iodobenzoic acid (VI),via activation with isobutyl chloroformate,furnishes the iodobenzamide (VII).Subsequent coupling of iodo amide (VII) with the ethynyl quinazoline (IV) employing Pd(PPh3)4 and CuI leads to the disubstituted acetylene (VIII).Catalytic hydrogenation of the triple bond in the presence of Pd/C affords (IX).Then,basic hydrolysis of phthalimido ester (IX) by means of Ba(OH)2 produces the target compound.