反应 #7010

反应方程式

4-(5-Methyl-[1,3,4]oxadiazol-2-yl)-piperidine-1-carboxylic acid tert-butyl ester

benzylamine

benzylamine

→

title compound

收率 70.4%

4-(4-Benzyl-5-methyl-4H-[1,2,4]triazol-3-yl)-piperidine-1-carboxylic acid tert-butyl ester

收率 70.4%

反应条件

后处理

1. 1
   温度The reaction mixture was cooled to room temperature
2. 2
   其他the reaction mixture was purified by chromatography on silica gel
3. 3
   其他The material isolated
4. 4
   其他was triturated with diethyl ether

实验过程

4-(5-Methyl-[1,3,4]oxadiazol-2-yl)-piperidine-1-carboxylic acid tert-butyl ester (5 g, 18.7 mmol) (see reference WO 0039125), benzylamine (2.5 ml, 22 mmol) and magnesium chloride (100 mg) were heated at 150° C. for 1 hour, a further quantity of benzylamine (2.5 ml, 22 mmol) was added and the mixture was heated at 150° C. for 4 hours. The reaction mixture was cooled to room temperature and the reaction mixture was purified by chromatography on silica gel using methanol in dichloromethane as eluant (3:97). The material isolated was triturated with diethyl ether to give the title compound as a white solid (4.69 g).

来源