KRP-199

2-喹喲沙林羧酸,7-[4-[[[[[(4-羧苯基)氨基]羰基]甲基]-1H-吡唑-1-基]-3,4-二氢-3-氧-6-(三氟甲基)-Chemical Name: 7-[4-[N-(4-Carboxyphenyl)carbamoyloxymethyl]-1H-imidazol-1-yl]-3-oxo-6-(trifluoromethyl)-3,4-dihydroquinoxaline-2-carboxylic acid
CAS No. 221164-28-9
项目整合开发状态: Preclinical
项目研究机构: Kyorin (Originator)
合成路线:The condensation between 5-acetamido-2-fluoro-4-nitrobenzotrifluoride (I) and 4-(hydroxymethyl)imidazole (II) in acetonitrile at 120 C in a sealed vessel furnished aryl imidazole (III).Subsequent acetamide hydrolysis in (III) with aqueous HCl provided nitro amine (IV),which was further reduced to phenylenediamine (V) by catalytic hydrogenation over Pd/C.Quinoxaline (VII) was prepared by condensation of phenylenediamine (V) with diethyl oxomalonate (VI) in boiling EtOH.The primary hydroxyl group of (VII) was then condensed with ethyl 4-isocyanatobenzoate (VIII) yielding carbamate (IX).Finally,both ethyl ester groups of (IX) were hydrolyzed by means of KOH to produce the target dicarboxylic acid.