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nebracetam synthesis

4synthesis methods
2-Pyrrolidinone, 4-[[(methylsulfonyl)oxy]methyl]-1-(phenylmethyl)-

1373821-40-9
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nebracetam

97205-34-0
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Yield:97205-34-0 94%

Reaction Conditions:

with ammonia in methanol at 50; under 3750.38 Torr; for 8 h;

Steps:

16 Example 16

Take 0.50g 1-benzyl-5-oxopyrrolidine-3-carboxylic acid mesylate 4 in a certain amount of methanol solvent, accessThe liquid ammonia is subjected to an amination reaction, the reaction pressure is controlled at 0.5 MPa, the reaction temperature is 50° C., and the reaction temperature is maintained for 8 hours. After the reaction is completed, 5 ml of water and 0.60 g of sodium ethoxide are added thereto, heated to reflux, and the reaction process is monitored by TLC. After the reaction was completed, it was cooled to room temperature, extracted three times with dichloromethane, washed once with water, dried over anhydrous sodium sulfate, and suction-filtered. The filtrate was spin-dried to obtain neracetam 1 0.339 g, yield 94%, purity 99.5%.

References:

CN104402791,2017,B Location in patent:Paragraph 0054; 0055; 0056; 0057; 0058; 0059; 0060-0069