新产品编号:1455949

Chemical Name: 3-(3-Amidinobenzamido)-4-(4-tert-butylbenzamido)benzoic acid hydrochloride
项目整合开发状态: Preclinical
项目研究机构: Lilly (Originator)
合成路线:Regioselective coupling of methyl 3,4-diaminobenzoate (I) with 3-cyanobenzoyl chloride (II) afforded benzamide (III).Further coupling of (III) with 4-tert-butylbenzoyl chloride (IV) gave diamide (V).Conversion of the methyl ester group of (V) into the benzyl ester analogue (VII) was effected by hydrolysis with LiOH,followed by treatment of the resulting carboxylic acid (VI) with benzyl bromide.Addition of hydroxylamine to the cyano group of (VII) gave rise to amidoxime (VIII).Subsequent hydrogenation of (VIII) over Pd/C produced the title amidine.