1,2-Dichloroethane → HCID 86758314, compound

Participants

Reaction Steps

To a mixture of 3-((E)-2-(4-fluorophenyl)-3-(imidazol-1-yl)-prop-1-enyl)benzoic acid (0.50 g, 1.55 mmol; prepared as the product of step D in Example 1), EDC (0.30 g, 1.55 mmol) and HOBt (0.21 g, 1.55 mmol) in dichloromethane (20 ml) was added α-methyl methionine methyl ester (0.33 g, 1.55 mmol) and 4-methylmorpholine (0.17 ml, 1.55 mmol). The solution was stirred at room temperature for 17 hrs, washed with brine (3×40 ml) dried over (MgSO4) and the solvent evaporated to leave a yellow gum. This was purified by chromatography (Biotage flash 40, 40 g SiO2 cartridge) eluting a gradient of 0-1% 0.88 aqueous ammonia/EtOAc to give the desired end product as a yellow gum 0.38 g (50%).

Provenance & Evidence