FR-183998

Chemical Name: N-(Diaminomethylene)-4-(2,5-dichlorothiophen-3-yl)-N'-[2-(dimethylamino)ethyl]isophthalamide dihydrochloride; 2-[5-(2,5-Dichlorothiophen-3-yl)-3-[N-[2-(dimethylamino)ethyl]carbamoyl]benzoyl]guanidine dihydrochloride
CAS No. 177733-06-1
项目整合开发状态: Preclinical
项目研究机构: Fujisawa (Originator)
合成路线:Mitsunobu coupling between boronic acid (I) and 3-bromo-2,5-dichlorothiophene (II) affords the thienyl isophthalate (III).Partial hydrolysis of diester (III) using methanolic KOH gives rise to mono-acid (IV),which is further condensed with N,N-dimethyl ethylenediamine (V) to provide the amide-ester (VI).Displacement of the methyl ester function of (VI) by guanidine (VII) then produces the target acyl guanidine,which is finally converted into the corresponding dihydrochloride salt.