反应详情

In THF (10 mL) were dissolved 2-(3-azabicyclo[3.1.0]hexan-3-yl)-4-((3-chloro-4-methoxybenzyl)amino)-pyrimidine-5-carboxylic acid (150 mg, 0.40 mmol) and 2-morpholinylethylamine (59 mg, 0.45 mmol). HATU (190 mg, 0.50 mmol) and triethylamine (101 mg, 1 mmol) were then added. The reaction was conducted at ambient temperature for 4 h. Then the reaction mixture was diluted with water and extracted with DCM. The organic phase was dried, concentrated, and purified by silica gel column chromatography (DCM/methanol=20/1) to give 2-(3-azabicyclo[3.1.0]hexan-3-yl)-4-((3-chloro-4-methoxybenzyl)amino)-N-(2-morpholinylethyl)pyrimidine-5-formamide as a white solid (71 mg, 36.5% yield).

1. extractionextracted with DCM
2. customThe organic phase was dried
3. concentrationconcentrated
4. custompurified by silica gel column chromatography (DCM/methanol=20/1)