تفاعل #342525

معادلة التفاعل

1-[2-(4-aminopiperidin-1-yl)ethyl]-7-fluoroquinoxalin-2(1H)-one

Intermediate 140

1-[2-(4-aminopiperidin-1-yl)ethyl]-7-fluoroquinoxalin-2(1H)-one

5-fluoro-1H-indole-2-carboxylic acid

N-(3-Dimethylaminopropyl)-N-ethylcarbodiimide

1-Hydroxybenzotriazole hydrate

→

title compound

المردود 79.6%

5-Fluoro-N-{1-[2-(7-fluoro-2-oxoquinoxalin-1(2H)-yl)ethyl]piperidin-4-yl}-1H-indole-2-carboxamide

المردود 79.6%

المذيبات

dichloromethane DMF

ظروف التفاعل

المعالجة

1. 1
   أخرىThe solvent was removed under reduced pressure
2. 2
   workup.STIRRINGstirred for 45 minutes
3. 3
   ترشيحfiltered

الإجراء التجريبي

A mixture of 1-[2-(4-aminopiperidin-1-yl)ethyl]-7-fluoroquinoxalin-2(1H)-one (Intermediate 140, 130 mg, 0.448 mmol), 5-fluoro-1H-indole-2-carboxylic acid (96.3 mg, 0.538 mmol), N-(3-Dimethylaminopropyl)-N-ethylcarbodiimide (EDC)(124 mg, 0.645 mmol) and 1-Hydroxybenzotriazole hydrate (HOBT) (87 mg, 0.645 mmol) in dichloromethane/DMF (4:1, 10 mL) was stirred for 2.5 hours at room temperature. The solvent was removed under reduced pressure and the residue was suspended in methanol, stirred for 45 minutes and then filtered to give title compound (161 mg).

المصدر