تفاعل #1605834

معادلة التفاعل

aripiprazole

triethylamine

benzyl isocyanate

→

N-benzyl-7-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butoxy)-2-oxo-3,4-dihydroquinoline-1(2H)-carboxamide

المذيبات

dichloromethane

ظروف التفاعل

المعالجة

1. 1
   أخرىThe reaction was quenched with water
2. 2
   استخلاصextracted with dichloromethane (3×20 mL)
3. 3
   غسيلwashed with brine (20 mL)
4. 4
   تجفيفdried over MgSO4
5. 5
   تركيزconcentrated
6. 6
   أخرىThe residue was purified by column chromatography on silica eluting with 0-10% tetrahydrofuran in ethyl acetate
7. 7
   أخرىThe product was triturated in heptane
8. 8
   أخرىto remove aliphatic impurities
9. 9
   ترشيحfiltered
10. 10
    أخرىdried
11. 11
    أخرىto afford Compound-79 (0.575 g) as a colorless solid

الإجراء التجريبي

To a solution of aripiprazole (1.5 g, 3.35 mmol) in dichloromethane (33 mL) was added triethylamine (0.56 mL, 4.01 mmol) and benzyl isocyanate (0.82 mL, 6.69 mmol). The reaction was stirred at room temperature for 48 hours. The reaction was quenched with water and extracted with dichloromethane (3×20 mL). The organics were combined, washed with brine (20 mL), dried over MgSO4 and concentrated. The residue was purified by column chromatography on silica eluting with 0-10% tetrahydrofuran in ethyl acetate. The product was triturated in heptane to remove aliphatic impurities and then filtered and dried to afford Compound-79 (0.575 g) as a colorless solid.

المصدر