RG-1103

Chemical Name: 1-(4-Benzylpiperidin-1-yl)-1-(6-hydroxy-1H-benzimidazol-2-yl)methanone
CAS No. 420136-91-0
项目整合开发状态: Preclinical
项目研究机构: Gedeon Richter (Originator)
合成路线:Treatment of the N-aryl oxalamic acid ethyl ester (I) with butylamine in toluene provides the oxalic diamide (II).The nitro group of (II) is then reduced to the corresponding amine (III) by catalytic hydrogenation over Pd/C.Subsequent thermal cyclization of the N-acyl phenylenediamine (III) leads to benzimidazole (IV).Hydrolysis of both the methyl ether and amide functions of (IV) with concentrated HBr furnishes 6-hydroxy-1H-benzimidazole-2-carboxylic acid (V).Then,coupling of acid (V) with 4-benzylpiperidine (VI) in the presence of TBTU gives rise to the desired amide