RO-09-8325

Chemical Name: 1-(1-Allyl-1H-benzimidazol-2-yl)-1-[3-methyl-4-[3-(pyridin-3-ylmethylamino)propoxy]-1-benzofuran-2-yl]methanone
CAS No. 445510-12-3
项目整合开发状态: Preclinical
项目研究机构: Chugai (Originator)
合成路线:Alkaline hydrolysis of ester (I),followed by chlorination of the resulting carboxylic acid (II) by means of oxalyl chloride furnishes the acid chloride (III).This is then treated with morpholine (IV) to provide the corresponding amide (V).Displacement of the bromide group of (V) with 3-(aminomethyl)pyridine (VI) leads to the secondary amine (VII),which is further protected as the N-Boc derivative (VIII) employing di-tert-butyl dicarbonate.Addition of the 2-lithiated benzimidazole (IX) to the morpholine amide (VIII) gives rise to ketone (X).The N-Boc group of (X) is finally cleaved by treatment with trifluoroacetic acid in CH2Cl2.