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912635-60-0

Ethyl 5-benzyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole-3-carboxylate synthesis

2synthesis methods
ethyl 2-(1-benzyl-4-oxopyrrolidin-3-yl)-2-oxoacetate

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Ethyl 5-benzyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole-3-carboxylate

912635-60-0
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Yield:912635-60-0 38.6 %

Reaction Conditions:

with hydrazine hydrate;acetic acid at 110;

Steps:

4.2 second step 5-Benzyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole-3-carboxylic acid ethyl ester 4c

Compound 4b (2.1g, 7.62mmol) was dissolved in the solvent acetic acid (60mL), hydrazine hydrate (539.1mg, 9.15mmol, 85% purity) was added, heated to 110°C for 5 hours, the reaction solution was concentrated under reduced pressure and then added with water Dilute, adjust the pH to about 8 with 2N sodium hydroxide, extract with ethyl acetate (50mL×3), combine the organic phases, dry with anhydrous sodium sulfate, filter to remove the desiccant, and concentrate the filtrate under reduced pressure. Purification by chromatography with eluent system A afforded the title compound 4c (800 mg, yield: 38.6%).

References:

CN115403595,2022,A Location in patent:Paragraph 0340-0343; 0348-0351