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
- 50 °C
PROCEDURE
实验过程
tert-butyl 4-(4-aminoisothiazol-5-yloxy)piperidine-1-carboxylate (1D4) (47 mg, 0.156 mmol), 5-amino-2-(2,6-difluorophenyl)thiazole-4-carboxylic acid (1E) (40 mg, 0.156 mmol), HATU (71 mg, 0.187 mmol) and DIEA (84 μL, 0.468 mmol) were mixed in DMF (5 mL), stirred at 50° C. for 1 hour, cooled to room temperature, diluted with ethyl acetate (50 mL), washed with brine, dried over Na2SO4, and concentrated in vacuo at room temperature (25° C.). The residue was purified with flash column (eluent: 10-30% ethyl acetate/petroleum ether) to afford the product tert-butyl 4-(4-(5-amino-2-(2,6-difluorophenyl)thiazole-4-carboxamido)isothiazol-5-yloxy)piperidine-1-carboxylate (1A) (17 mg, 0.031 mmol).
WORKUP
后处理
- temperaturecooled to room temperature
- washwashed with brine
- dry with materialdried over Na2SO4
- concentrationconcentrated in vacuo at room temperature (25° C.)
- customThe residue was purified with flash column (eluent: 10-30% ethyl acetate/petroleum ether)