反应详情

To a solution of 81 mg (S)-2-({5-[2-((S)-2-(2-Fluoroethyl-carbamoyl)-pyrrolidin-1-yl)-2-oxo-ethoxy]-1-phenyl-1H-pyrazole-3-carbonyl}-amino)-pentanedioic acid 5-tert-butyl ester in 5 ml DMF were added 22 μl DIPEA, 52 mg HATU and 24 mg (R)-2-Methyl-piperazine-1-carboxylic acid ethyl ester. After stirring for 24 h the solution was concentrated, the residue dissolved in 1.5 ml dichloromethane and treated with 300 μl TFA. After stirring for 16 h the solvents were removed under reduced pressure and the residue purified by preparative HPLC (C18 reverse phase column, elution with a water/MeCN gradient with 0.1% TFA). The fractions containing the product were lyophilized to yield the pure product.

1. concentrationwas concentrated
2. dissolutionthe residue dissolved in 1.5 ml dichloromethane
3. additiontreated with 300 μl TFA
4. stirringAfter stirring for 16 h the solvents
5. customwere removed under reduced pressure
6. customthe residue purified by preparative HPLC (
7. washC18 reverse phase column, elution with a water/MeCN gradient with 0.1% TFA)
8. additionThe fractions containing the product
9. customto yield the pure product