Electric Literature of 87941-55-7, These common heterocyclic compound, 87941-55-7, name is 4-Bromo-1-trityl-1H-imidazole, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.
To a suspension of 3.00 g (7.71 mmol) of 4-bromo-1-trityl-1H-imidazoie in 30 ml of dioxane1.58 g (9.23 mmol) of 4-methoxymethyi boronic acid, 3.47 g (10.5 mmol) of cesiumcarbonate and 0.121 g (0.131 mmol) of tris-(dibenzylideneaceton)dipalladium are added, followed by 0.315 ml (0.308 ml) of a solution of 5 g of tri-t-buylphosphine in 25 ml of dioxane. The mixture is heated at 80C and stirred for 6.5 hours. After cooling to room temperature the suspension is diluted with dichloromethane and filtered, the filter cake washed with ethyl acetate and the filtrate concentrated to dryness. The residue is purified by flash chromatography on silica (40 – 63 urn particle size) with hexane / ethyl acetate 7:3, yielding 2.805 g of 4-(4-methoxymethyl-phenyl)-1-trityl-1H-imidazole, Rt = 4.659 min by HPLC on a nucleosil C18HD column with acetonitril + 0.05% TFA / water + 0.05% TFA, 20/80 to 100/0 over 6 min, 1.0 ml/min solvent flow. MS (API-ES, pos. scan): e/m = 431 (M+1).
Statistics shows that 4-Bromo-1-trityl-1H-imidazole is playing an increasingly important role. we look forward to future research findings about 87941-55-7.
Reference:
Patent; NOVARTIS AG; NOVARTIS PHARMA GMBH; WO2006/10591; (2006); A2;,
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem