Triethylamine → 1-{2-[{6-[(5-Bromopyrimidin-2-yl)amino]hexanoyl}(methyl)amino]ethyl}piperidin-4-yl biphenyl-2-ylcarbamate

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Reaction Steps

5-Bromo-2-chloropyrimidine (124 mg, 0.643 mmol) and the compound (300 mg, 0.643 mmol) obtained in Example 1a were dissolved in n-butanol (5 mL), triethylamine (0.134 mL, 0.965 mmol) was added, and the mixture was stirred with heating to reflux for 19 hours. The solvent was evaporated under reduced pressure, and the resulting residue was purified by NH silica gel column chromatography (hexane:ethyl acetate=1:1→0:100, v/v) to give the title compound (299 mg; yield, 75%) as a yellow solid.

Provenance & Evidence