تفاعل #1702118

معادلة التفاعل

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

hydrogen chloride

triethylamine

3-nitrobenzoyl chloride

→

desired product

المردود 70.0%

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

المردود 70.0%

المذيبات

THF

ظروف التفاعل

المعالجة

1. 1
   تركيزconcentrated under vacuum
2. 2
   أخرىThe residue was partitioned in EtOAc
3. 3
   تجفيفThe organic layer was dried over Na2SO4
4. 4
   ترشيحfiltered
5. 5
   تركيزconcentrated under vacuum

الإجراء التجريبي

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.

المصدر