BIIB-513

Chemical Name: N2-[4-[4-(2-Furylcarbonyl)piperazin-1-yl]-3-(methylsulfonyl)benzoyl]guanidine methanesulfonate
CAS No. 193401-08-0 (mono HCl salt)
项目整合开发状态: Preclinical
项目研究机构: Boehringer Ingelheim (Originator)
合成路线:Condensation of N-(2-furanylcarbonyl)piperazine (I) with 4-chloro-3-(methylsulfonyl)benzoic acid (II) at 120 C produced the disubstituted piperazine (III).After activation of the carboxy group as the imidazolide (IV) upon treatment with 1,1'-carbonyldiimidazole and N-methylmorpholine,treatment with guanidine hydrochloride (V) and NaH in hot DMF yielded the corresponding benzoyl guanidine,which was finally isolated as the methanesulfonate salt.