反应详情

To a mixture of (R)-5-(4-cyano-benzyl)-7-(3,5-dichloro-phenyl)-5-methyl-6-oxo-6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-carboxylic acid (80 mg, 0.18 mmol) and 4-amino-4-(1-pyridin-2-yl-cyclopropylcarbamoyl)-piperidine-1-carboxylic acid tert-butyl ester (74 mg, 0.20 mmol) in DMF (1 mL) was added HATU (76 mg, 0.19 mmol) and diisopropylethylamine (47 mg, 0.36 mmol). The reaction was stirred at room temperature for 7 h. After addition of water (10 mL) the mixture was extracted with EtOAc (2×15 mL). The organic layer was washed with brine and dried over Na2SO4. The solvent was removed in vacuo and the remaining residue was purified via reverse phase HPLC to afford 4-{[(R)-5-(4-cyanobenzyl)-7-(3,5-dichlorophenyl)-5-methyl-6-oxo-6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-carbonyl]-amino}-4-(1-pyridin-2-yl-cyclopropyl-carbamoyl)-piperidine-1-carboxylic acid tert-butyl ester as a white solid (140 mg), m/z 784.9 [M+1]+.

1. extractionwas extracted with EtOAc (2×15 mL)
2. washThe organic layer was washed with brine
3. dry with materialdried over Na2SO4
4. customThe solvent was removed in vacuo
5. customthe remaining residue was purified via reverse phase HPLC