5-Fluoroindole-2-carboxylic acid → (2S)-2-[(5-fluoro-1H-indole-2-carbonyl)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 (605 mg, 0.8 mmol, example 109, step A) as described for example 109 (step B) using 5-fluoroindole-2-carboxylic acid (222 mg, 1.24 mmol) instead of N-(4-fluorobenzyl)indole-2-carboxylic acid. The crude material was purified by flash chromatography using 10, 20 and 40% EtOAc/CH2Cl2 as the eluent. The title compound was obtained as yellow crystals (400 mg, 72%).

Provenance & Evidence