4-Bromoaniline → (E)-[2-(3-{4-[1-(4-Bromo-phenylcarbamoyl)-3-(tert-butyl-dimethyl-silanyloxy)-propyl]-phenyl}-acryloylamino)-phenyl]-carbamic acid tert-butyl ester

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To a solution of (E)-2-{4-[2-(2-tert-butoxycarbonylamino-phenylcarbamoyl)-vinyl]-phenyl}-4-(tert-butyl-dimethyl-silanyloxy)-butyric acid (2.5 g, 4.52 mmol), EDCI (1.2 g, 4.97 mmol) and HOBt (671 mg, 4.97 mol) in CH2Cl2 (50 mL) was added 4-bromo-phenylamine (786 mg, 4.57 mmol). This mixture was stirred overnight at room temperature and then diluted with CH2Cl2 (50 mL), washed with saturated aqueous NaHCO3 solution, water and brine, dried with Na2SO4, and evaporated to obtain a yellow residue. MS: calc'd 708 (MH+), exp 708 (MH+).

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