反应详情

To a stirred mixture of (S)-2-[4-(4-Amino-phenyl)-thiazol-2-ylcarbamoyl]-pyrrolidine-1-carboxylic acid benzyl ester (Compound 5050, Example 50, 0.06 g, 0.14 mmol) in DCM (2.0 mL) at 0° C. was added TEA (0.0.025 mL) followed by addition of cyclopropanesulfonyl chloride (0.016 mL). The reaction mixture was stirred at room temperature for 1 h then was concentrated in vacuo to give the crude product. Purification of the crude product by reverse phase HPLC furnished the desired product. 1HNMR (DMSO-d6) δ(ppm) 7.87-7.83 (m, 2H), 7.37-7.07 (m, 7H), 5.17-5.13 (m, 2H), 4.89-4.87 (m, 3H), 4.52-4.47 (m, 1H), 3.69-3.54 (m, 2H), 2.60-2.56 (m, 1H), 2.38-2.35 (m, 1H), 2.08-1.96 (m, 3 H), 1.07-0.95 (m, 4H); MS: 527.1 (M+H+).

1. additionwas added TEA (0.0.025 mL)
2. concentrationthen was concentrated in vacuo
3. customto give the crude product
4. customPurification of the crude product by reverse phase