3,4-Di-(4-fluorobenzyloxy)benzoic acid → (2S)-2-[[3,4-bis[(4-fluorophenyl)methoxy]benzoyl]amino]-N-(3-hydroxy-4-methoxy-phenyl)-N'-trityl-pentanediamide

Participants

Reaction Steps

The title compound was prepared from N-[Nα-(9-fluorenylmethoxycarbonyl)-Nδ-trityl-L-glutaminyl]-3-hydroxy-4-methoxyaniline (642 mg, 0.9 mmol, example 109, step A) as described for example 109 (step B) using 3,4-di-(4-fluorobenzyloxy)benzoic acid (485 mg, 1.3 mmol) instead of N-(4-fluorobenzyl)indole-2-carboxylic acid. The crude material was purified by flash chromatography using successively 5%, 10% and 30% EtOAc/CH2Cl2 as the eluent. The title compound was obtained as white crystals (260 mg, 34%).

Provenance & Evidence