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1-METHYL-3,4-DIHYDROPYRROLO[1,2-A]-PYRAZINE synthesis

3synthesis methods
-

Yield:64608-66-8 87%

Reaction Conditions:

with trichlorophosphate at 0;Reflux;

Steps:

6.2 Step 2: Preparation of 1-methyl-3,4-dihydropyrrolo[1,2-a]pyrazine

N-(2-(1H-pyrrol-1-yl)ethyl)acetamide (3.92 g, 25.8 mmol) was added portionwise to phosphorus oxychloride (40 mL) at 0 ° C. After graduation, The reaction mixture was refluxed overnight. The reaction mixture was cooled to room temperature, The organic solvent was removed by steam distillation under reduced pressure. The crude product was added with a saturated aqueous solution of sodium hydrogencarbonate, adjust the pH 7 ~ 8, The aqueous phase was extracted with dichloromethane / isopropanol (85:15) (50 mL x 3) The combined organic phases were washed with saturated brine (100 mL) Dried over anhydrous sodium sulfate and purified by silica gel column chromatography (eluent: dichloromethane / methanol = 100% to 90%) to give 1-methyl-3,4-dihydropyrrolo[1,2-a]pyrazine (3 g, yield 87%).

References:

CN106279160,2017,A Location in patent:Paragraph 0325; 0332; 0333; 0334