新产品编号:2294409

Chemical Name: N-[3-(4-Chlorophenyl)-3-(2-pyridyl)propyl]-4-(1H-imidazol-4-ylmethyl)benzamidine
项目整合开发状态: Preclinical
项目研究机构: Schering-Plough (Originator)
合成路线:The unsaturated nitrile (III) is prepared by Wittig reaction of 2-(4-chlorobenzoyl)pyridine (I) with phosphorane (II).Subsequent reduction of (III) with NaBH4 in boiling isopropanol provides the saturated nitrile (IV).The cyano group of (IV) is then reduced to amine (V) employing LiAlH4 in refluxing Et2O.

合成路线:Metalation of 1-trityl-4-iodoimidazole (VI) with ethylmagnesium bromide,followed by addition to 4-cyanobenzaldehyde (VII) gives rise to the carbinol (VIII),which is further reduced to the diaryl methane (IX) employing triibutyltin hydride in the presence of AIBN.Trimethylaluminium-catalyzed coupling between nitrile (IX) and amine (V) provides amidine (X).The N-trityl group of (X) is finally removed under acidic conditions to furnish the title compound.