RWJ-67657

4-(4-氟苯基)-2-(4-羟基-1-丁炔)-1-(3-苯基丙基)-5-(4-吡啶基)咪唑Chemical Name: 4-[4-(4-Fluorophenyl)-1-(3-phenylpropyl)-5-(4-pyridinyl)-1H-imidazol-2-yl]-3-butyn-1-ol
CAS No. 215303-72-3
项目整合开发状态: Phase I
项目研究机构: R.W. Johnson (Originator)
合成路线:Selenium dioxide oxidation of diaryl ethanone (I) afforded diketone (II),which was cyclized to the imidazole (III) by reaction with hexamethylenetetramine and ammonium acetate in hot AcOH.Alkylation of (III) with 1-bromo-3-phenylpropane (IV) in the presence of NaH gave rise to a mixture of regioisomeric imidazoles (V) and (VI) that were separated by column chromatography.After deprotonation of the desired isomer (V) with LDA,treatment with iodine produced iodoimidazole (VII).Then,palladium-catalyzed coupling of (VII) with 3-butyn-1-ol (VIII) yielded the title compound.