반응 #1532283

반응 방정식

7-(3,4-dihydro-1H-isoquinolin-2-yl)-2,3-dimethyl-1H-pyrrolo[2,3-c]pyridin-5-carboxylic acid

1-hydroxybenzotriazole hydrate

1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride

diisopropylethylamine

piperidine

→

titled compound

수율 50.0%

[7-(3,4-dihydro-1H-isoquinolin-2-yl)-2,3-dimethyl-1H-pyrrolo[2,3-c]pyridin-5-yl]-(piperidin-1-yl)-methanone

수율 50.0%

용매

dichloromethane

반응 조건

후처리

1. 1
   농축concentrated under reduced pressure
2. 2
   기타The resulting residue was purified with silica gel column chromatography (ethyl acetate/n-hexane=1/1

실험 절차

A solution of 7-(3,4-dihydro-1H-isoquinolin-2-yl)-2,3-dimethyl-1H-pyrrolo[2,3-c]pyridin-5-carboxylic acid (450 mg, 1.4 mmol) prepared in Step 1, 1-hydroxybenzotriazole hydrate (284 mg, 2.1 mmol), 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (401 mg, 2.1 mmol), diisopropylethylamine (730 μl, 4.2 mmol), and piperidine (270 μl, 2.1 mmol) in dichloromethane (5 ml) was stirred overnight at room temperature and then concentrated under reduced pressure. The resulting residue was purified with silica gel column chromatography (ethyl acetate/n-hexane=1/1, v/v) to give 250 mg of the titled compound as a white solid. (Yield: 50%).

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