反应详情

To a solution of 1.0 g 4-[(R)-2-((S)-2-Cyclobutylcarbamoyl-pyrrolidin-1-yl)-1-methyl-2-oxo-ethoxy]-7-methyl-quinoline-2-carboxylic acid in 30 ml DMF were added 1.2 g DIPEA, 319 mg HOAt and 450 mg EDC. After 5 minutes 1.1 g 4-((S)-2-Amino-4-benzyloxy-butyryl)-piperazine-1-carboxylic acid butyl ester hydrotrifluoroacetate were added and the mixture stirred for 16 h. The mixture was concentrated, diluted with DCM and washed with aqueous LiCl (4%), saturated aqueous NaHCO3 and brine. The crude product was used in the next reaction step. Yield: 2.8 g.

1. concentrationThe mixture was concentrated
2. additiondiluted with DCM
3. washwashed with aqueous LiCl (4%), saturated aqueous NaHCO3 and brine
4. customThe crude product was used in the next reaction step