反应 #1702118

反应方程式

N-(3-aminobenzyl)-2,5-dichloropyrimidin-4-amine

hydrogen chloride

triethylamine

3-nitrobenzoyl chloride

→

desired product

收率 70.0%

N-(3-{[(2,5-Dichloropyrimidin-4-yl)amino]methyl}phenyl)-3-nitrobenzamide

收率 70.0%

溶剂

THF

反应条件

后处理

1. 1
   浓缩concentrated under vacuum
2. 2
   其他The residue was partitioned in EtOAc
3. 3
   干燥The organic layer was dried over Na2SO4
4. 4
   过滤filtered
5. 5
   浓缩concentrated under vacuum

实验过程

To a mixture of N-(3-aminobenzyl)-2,5-dichloropyrimidin-4-amine.hydrogen chloride (0.10 g, 0.29 mmol) (prepared according to Example 3, step B) and triethylamine (0.16 mL, 1.2 mmol) in THF (3 mL) was added slowly 3-nitrobenzoyl chloride (54 mg, 0.29 mmol). The resulting mixture was stirred at rt for 2 hours and concentrated under vacuum. The residue was partitioned in EtOAc and water. The organic layer was dried over Na2SO4, filtered, and concentrated under vacuum to give the desired product as a yellow solid (90 mg, 70%). LCMS for C18H14Cl2N5O3 (M+H)+: m/z=418.0, 420.0.

来源