Continuously updated synthesis method about C8H13N3O

The synthetic route of 1157012-67-3 has been constantly updated, and we look forward to future research findings.

1157012-67-3, name is 1-(Tetrahydro-2H-pyran-4-yl)-1H-pyrazol-5-amine, 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. Formula: C8H13N3O

1005451 To a mixture of 2-(tetrahydro-pyran-4-yl)-2H-pyrazol-3-ylamine (5.34 g, 32 mmol) in EtOH (150 mL) was added 2-ethoxymethylene-malonic acid diethyl ester (8.29 g, 38.4 mmol). The resulting mixture was stirred at 80 C overnight. The mixture was concentrated under reduced pressure and the residue was purified by silica gel column chromatography (from 100% PE to PE/EA = 25/1) to afford 2-{[2-(tetrahydro-pyran-4-yl)-2H-pyrazol-3-ylamino]-methylene}malonic acid diethyl ester (430 mg, two-step yield: 3%) as a white solid. MS: m/z 338.1 (M+H).

The synthetic route of 1157012-67-3 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; SANFORD-BURNHAM MEDICAL RESEARCH INSTITUTE; PINKERTON, Anthony, B.; HASSIG, Christian, A.; JACKSON, Michael, R.; ARDECKY, Robert, John; PASS, Ian; (436 pag.)WO2016/123392; (2016); A2;,
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics