反应详情
EQUATION
反应方程式
REACTANTS
反应物
PRODUCTS
生成物
AUXILIARIES
试剂、催化剂与溶剂
CONDITIONS
反应条件
- 温度
- 25 °C
PROCEDURE
实验过程
To a solution of (S)-1-((4-(2,5-difluoro-4-(1-((4-fluorophenyl)carbamoyl)cyclopropanecarboxamido)phenoxy)pyridin-2-yl)amino)-1-oxopropan-2-yl acetate (180 mg, 0.323 mmol) in a solution of MeOH—H2O (3:1, 20 mL) was added potassium carbonate (111.6 mg, 0.809 mmol), the mixture was stirred at 25° C. for 12 h. The reaction mixture was concentrated and purified by prep-TLC to give (S)—N-(2,5-difluoro-4-((2-(2-hydroxypropanamido)pyridin-4-yl)oxy)phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide (100 mg, 60% yield). 1H NMR (400 MHz, Methanol-d4): δ 8.21-8.16 (m. 2H), 7.78 (d, J=2.4 Hz, 1H), 7.54-7.51 (m, 2H), 7.28-7.24 (m, 1H), 7.10-7.05 (m, 2H), 6.76-6.74 (dd, J=6.0, 2.4 Hz, 1H), 4.23 (q, J=6.8 Hz, 1H), 1.75-1.67 (m, 4H), 1.39 (d, J=6.8 Hz, 3H); MS (ESI): m/z 515.2 [M+H]+.
WORKUP
后处理
- concentrationThe reaction mixture was concentrated
- custompurified by prep-TLC