E-6039, E-6006 citrate

N,N-二甲基-N-[2-[1-(1-甲基-1H-吡氮醇-5-基)-1-(2-哧基)甲氧基]乙基]胺柠檬酸盐Chemical Name: N,N-Dimethyl-N-[2-[1-(1-methyl-1H-pyrazol-5-yl)-1-(2-thienyl)methoxy]ethyl]amine citrate
CAS No. 247046-64-6, 247046-62-4 (free base)
项目整合开发状态: Phase I
项目研究机构: Esteve (Originator)
合成路线:Lithiation of N-methylpyrazole (I) by means of n-butyllithium,followed by addition to 2-thiophenecarboxaldehyde (II),afforded carbinol (III).This compound was alternatively obtained by sodium borohydride reduction of diheteroaryl ketone (IV).Condensation of alcohol (III) with either 2-(dimethylamino)ethyl chloride (IV) in the presence of NaOH or 2-(dimethylamino)ethanol (VI) under catalysis of H2SO4 furnished ether (VII).This compound was finally converted to the title citrate salt by treatment with citric acid in EtOH.