新产品编号:2289663

Chemical Name: N-Methyl-N-[2-[2-[2-(methylamino)vinyl]-4-[1-methyl-4-(3,4,5-trimethoxyphenyl)-1H-imidazol-5-yl]phenyl]vinyl]amine hydrochloride
项目整合开发状态: Preclinical
项目研究机构: Abbott (Originator)
合成路线:The condensation between 3,4,5-trimethoxybenzaldehyde (I),4-methylbenzenesulfinic acid (II) and formamide in the presence of camphorsulfonic acid gave tosyl-(3,4,5-trimethoxyphenyl)methylformamide (III),which was subsequently dehydrated to the isonitrile (IV) by treatment with POCl3 and Et3N.After conversion of 4-methoxy-3-nitrobenzaldehyde (V) to the corresponding imine with methylamine,its reaction with the tosylmethyl isonitrile (IV) gave rise to the diaryl imidazole (VI).The nitro group of (VI) was finally reduced to amine by using SnCl2 and HCl or ammonium formiate and Pd/C

合成路线:The condensation of 3,4,5-trimethoxybenzaldehyde (I) with 4-methylphenylsulfinic acid (II) and formamide by means of hot CSA gives the adduct (III),which is treated with POCl3 in DME to yield the isonitrile (IV).The reaction of benzaldehyde (V) with methylamine and AcOH in refluxing ethanol gives the enamine (VI),which is finally cyclized with isonitrile (IV) by means of K2CO3 in ethanol/DME to afford the target 1-methylimidazole.