Triethylamine → Pyrimidine-5-carboxylic acid{1-[2-chloro-4-(2-chloro-4-hydroxy-phenoxy)-benzylcarbamoyl]-cyclopropyl}-amide

Participants

Reaction Steps

269 μl (1.93 mmol) of triethylamine and 166 mg (0.52 mmol) of TBTU were added to a solution of 100 mg (0.48 mmol) of 1-[(pyrimidin-5-carbonyl)-amino]-cyclopropanecarboxylic acid (from 1b) in 5 mL DMF and the mixture was stirred for 10 min at RT. Then 147 mg (0.37 mmol) of 4-(4-aminomethyl-3-chloro-phenoxy)-3-chloro-phenol-trifluoroacetic acid salt dissolved in 30 mL THF was added. The reaction mixture was stirred for 2 h at RT and evaporated to dryness. The residue was purified by chromatography (reversed phase).

Provenance & Evidence