تفاعل #73030

معادلة التفاعل

4-aminomethyltetrahydropyran-4-ol

4-chloro-3-nitro[1,5]naphthyridine

triethylamine

→

4-[(3-nitro[1,5]naphthyridin-4-ylamino)methyl]tetrahydropyran-4-ol

المردود 93.7%

المذيبات

dichloromethane

dichloromethane

ظروف التفاعل

المعالجة

1. 1
   تركيزit was concentrated under reduced pressure
2. 2
   workup.STIRRINGThe residue was stirred with water (300 mL)
3. 3
   أخرىThe resulting solid was isolated by filtration
4. 4
   غسيلrinsed with water
5. 5
   أخرىdried in a vacuum oven at 50° C. for 4 hours

الإجراء التجريبي

A solution of 4-chloro-3-nitro[1,5]naphthyridine (16.6 g, 79.0 mmol) in dichloromethane (250 mL) and triethylamine (14.3 mL, 102.7 mmol) was cooled to 4° C. A solution of 4-aminomethyltetrahydropyran-4-ol (11.4 g, 86.9 mmol) in dichloromethane (70 mL) was added dropwise over a period of 30 minutes. The reaction mixture was allowed to stir at ambient temperature over the weekend and then it was concentrated under reduced pressure. The residue was stirred with water (300 mL). The resulting solid was isolated by filtration, rinsed with water, and dried in a vacuum oven at 50° C. for 4 hours to provide 22.53 g of 4-[(3-nitro[1,5]naphthyridin-4-ylamino)methyl]tetrahydropyran-4-ol.

المصدر