反应详情

温度

0 °C

1-Methylimidazole (38.2 μl, 0.479 mmol) was added into a solution of (3S)-2-[(2R)-3-cyclopentyl-2-({formyl[(phenylmethyl)oxy]amino}methyl)propanoyl]-1-{[(phenylmethyl)oxy]carbonyl}-3-pyrazolidine carboxylic acid (100 mg, 0.240 mmol) in 1.0 ml of DMF. The solution was cooled to 0° C., and then mesyl chloride (24.26 μl, 0.311 mmol) was added dropwise at 0° C. 4-Aminopyrimidine (34.2 mg, 0.359 mmol) dissolved in another 1.0 ml of DMF was then added. The reaction mixture was stirred for 3.5 h at rt. The reaction mixture was concentrated and purified by RP-HPLC to afford (3S)-2-[(2R)-3-cyclopentyl-2-({formyl[(phenylmethyl)oxy]amino}methyl)propanoyl]-1-methyl-N-4-pyrimidinyl-3-pyrazolidinecarboxamide (95 mg, 0.192 mmol, 80%) as a white foam solid. LC-MS (ES) m/e 495.3 (M+H)+.

1. additionwas then added
2. concentrationThe reaction mixture was concentrated
3. custompurified by RP-HPLC