KCB-328

Chemical Name: N-[3-Amino-4-[2-[N-[2-(3,4-dimethoxyphenyl)ethyl]-N-methylamino]ethoxy]phenyl]methanesulfonamide hydrochloride
项目整合开发状态: Preclinical
项目研究机构: Chugai (Originator), Choongwae (Not Determined), Chung Wue (Licensee)
合成路线:Alkylation of phenol (I) with 1,2-dibromoethane (II) in the presence of K2CO3 in DMF yielded bromoethyl ether (III),which was further,condensed with amine (IV) to afford tertiary amine (V).The nitro group of (V) was then reduced by either catalytic hydrogenation in the presence of Pd/C or by treatment with SnCl2 in aqueous HCl,and the resulting aniline (VI) was condensed with methanesulfonyl chloride in pyridine to give sulfonamide (VII).Finally,acid hydrolysis of the acetamido group provided the title compound.
📌 参考资料/链接:
参考文献标题:Synthesis and biological activity of KCB-328 and its analogues: Novel class III antiarrhythmic agents with little reverse frequency dependence
文献作者:Kim,D.-I.; Kim,H.Y.; Kwon,L.S.; Park,S.D.; Jeon,G.H.; Jung,K.Y.; Min,J.K.; Nam,W.H.; Lee,K.; Chung,Y.S.; Tanabe,S.; Kozono,T.
参考来源:Bioorg Med Chem Lett 1999,9(1),85