Extracurricular laboratory: Synthetic route of 1280210-79-8

The synthetic route of 1280210-79-8 has been constantly updated, and we look forward to future research findings.

1280210-79-8, name is tert-Butyl 4,6-dihydropyrrolo[3,4-c]pyrazole-5(2H)-carboxylate, belongs to pyrazoles-derivatives compound, is considered to be a conventional heterocyclic compound, which is widely used in drug synthesis. The chemical synthesis route is as follows. Safety of tert-Butyl 4,6-dihydropyrrolo[3,4-c]pyrazole-5(2H)-carboxylate

Under N2 protection and a condition free of water and oxygen, Intermediate 2 (604 mg, 2.87 mmol) wasdissolved in tetrahydrofuran (20 ml), which was cooled to 0C, and sodium hydride (180 mg, 60 wt%, 4.5 mmol) wasadded, followed by stirring for 30 min. Cyclopropylsulfonyl chloride (1.27 g, 9.0 mmol) was added dropwise, and thetemperature was allowed to rise spontaneously to room temperature, followed by reaction for 1 hour. The reaction was quenched by addition of water (20 ml) to the reaction solution, which was then extracted with ethyl acetate (20 ml32).The organic phases were combined, dried over anhydrous sodium sulfate, concentrated, re-dissolved in 5 ml tetrahydrofuran,and cooled to -10C to 0C. Potassium t-butoxide (36 mg, 0.32 mmol) was added, and the reaction was allowedto proceed for 28 hours at this temperature. After the reaction was completed, an aqueous solution of citric acid (1 ml,15%) was added, and water (10 ml) was added. The solution was extracted with ethyl acetate (20 mL33). The organicphases were combined, dried over anhydrous sodium sulfate, and concentrated. The residue was purified by silica gelcolumn chromatography (petroleum ether/ethyl acetate (v/v) = 2:1) to obtain a white solid 1a (660 mg, yield 73%).

The synthetic route of 1280210-79-8 has been constantly updated, and we look forward to future research findings.