反应详情

To a solution of 193 mg 4-{2-[(5-Carboxymethoxy-1-phenyl-1H-pyrazole-3-carbonyl)-amino]-acetyl}-piperazine-1-carboxylic acid butyl ester in 2 ml DMF were added 150 mg HATU and 69 μl DIPEA. After 10 minutes a solution of 54 mg (S)-5-Pyrrolidin-2-yl-1H-tetrazole in 1 ml DMF was added and after 36 h the reaction mixture was diluted with dichloromethane and extracted with aqueous LiCl (4%), 0.1 M HCl and brine. The crude product thus obtained after evaporation of the solvent was purified by preparative HPLC (C18 reverse phase column, elution with a water/MeCN gradient with 0.1% TFA). The fractions containing the product were immediately lyophilized to yield the title compound

1. extractionextracted with aqueous LiCl (4%), 0.1 M HCl and brine
2. customThe crude product thus obtained
3. customafter evaporation of the solvent
4. customwas purified by preparative HPLC (
5. washC18 reverse phase column, elution with a water/MeCN gradient with 0.1% TFA)
6. additionThe fractions containing the product