반응 #1702118

반응 방정식

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

hydrogen chloride

triethylamine

3-nitrobenzoyl chloride

→

desired product

수율 70.0%

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

수율 70.0%

용매

THF

반응 조건

후처리

1. 1
   농축concentrated under vacuum
2. 2
   기타The residue was partitioned in EtOAc
3. 3
   건조The organic layer was dried over Na2SO4
4. 4
   여과filtered
5. 5
   농축concentrated under vacuum

실험 절차

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.

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