4-Iodobenzoic acid → 4-[3-(3-Tert-butyl-5-chloro-4-dimethylaminophenyl)-3-hydroxyprop-1-ynyl]benzoic acid

Participants

Reaction Steps

In a manner analogous to example 1 f, the process is carried out by a reaction of 200 mg (0.8 mmol) of 4-iodobenzoic acid with 300 mg (1.1 mmol) of 1-(3-tert-butyl-5-chloro-4-dimethylaminophenyl)prop-2-yn-1-ol in the presence of 8 mg (0.04 mmol) of copper iodide and 16 mg (0.02 mmol) of bis(triphenylphosphine)palladium chloride. 270 mg of 4-[3-(3-tert-butyl-5-chloro-4-dimethylaminophenyl)-3-hydroxyprop-1-ynyl]benzoic acid are obtained in the form of a whitish solid (Mp=120° C., yield=87%).

Provenance & Evidence