反应详情

To a solution of 5-amino-N-(5-((2S,5R,6R)-5-amino-6-fluorooxepan-2-yl)-1-methyl-1H-pyrazol-4-yl)-2-(cyclopent-1-en-1-yl)thiazole-4-carboxamide (Example 271) in methanol was added 10% palladium on carbon, and the mixture was stirred overnight under an atmosphere of hydrogen. The mixture was then filtered through Celite and concentrated in vacuo. HPLC purification provided 272. 1H NMR (400 MHz, DMSO-d6) δ 9.26 (s, 1H), 7.77 (s, 1H), 7.05 (s, 2H), 5.17-4.78 (m, 2H), 4.17-3.92 (m, 2H), 3.71 (s, 3H), 3.47-3.34 (m, 1H), 3.27-3.15 (m, 1H), 2.23-2.11 (m, 1H), 2.11-1.95 (m, 2H), 1.94-1.83 (m, 1H), 1.82-1.57 (m, 9H). LCMS (ES+) m/z 423 (M+1).

1. filtrationThe mixture was then filtered through Celite
2. concentrationconcentrated in vacuo
3. customHPLC purification