反应详情

(2-Nitrobenzyl)triphenylphosphonium bromide monohydrate (1.4 equiv), potassium carbonate (2.0 equiv) and 18-crown-6 (0.1 equiv) were combined in DME (0.16 M vs aldehyde). The mixture was stirred at room temperature for 5 min. tert-Butyl(2R,5S)-5-formyl-2-{2-[2-({(2S)-2-[(methoxycarbonyl)amino]-3,3-diphenylpropanoyl}amino)phenyl]ethyl}morpholine-4-carboxylate (1.0 equiv) was dissolved in DME (0.16 M) and added to the reaction mixture. The reaction mixture was stirred at room temperature for 18 h, filtered over solka floc and concentrated. The crude product was purified using automated silica-gel flash chromatography using a solvent gradient of 0% to 100% of ethyl acetate and hexanes.

1. additionadded to the reaction mixture
2. filtrationfiltered over solka floc
3. concentrationconcentrated
4. customThe crude product was purified