Application of 1260243-04-6,Some common heterocyclic compound, 1260243-04-6, name is Ethyl 5-amino-1H-pyrazole-4-carboxylate, molecular formula is C6H9N3O2, traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.
To a solution of ethyl 5-amino-lH-pyrazole-4-carboxylate (13.7 g, 88.0 mmol) in DMF (150 mL) was added ethyl (//)-3 -ethoxy aery late (15.2 g, 106.0 mmol) and the reaction mixture was stirred at 1 l0C for 1 h. The reaction mixture was diluted with water, adjusted pH to 2 with 2 N HC1 aqueous. The mixture was filtrated and the residue was washed with water and ethyl acetate and the filtrate was concentrated under reduced pressure to give the title compound as a white solid (18.3 g, 100 %), which used in next step without further purification. ‘H NMR (400 MHz, CDCb): d, 1.28 (t, J= 6.8Hz, 3H), 4.27 (q, J= 12 Hz, 2H), 6.15 (d, J= 7.6 Hz, 1H), 8.13 (s, 1H), 8.57 (d, J= 8.0 Hz, 1H), 11.74 (brs, 1H). ESI-MS (EI+, m/z): 208.1.
The synthetic route of 1260243-04-6 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; DANA-FARBER CANCER INSTITUTE, INC.; GRAY, Nathanael S.; HATCHER, John M.; POWELL, Chelsea E.; JANNE, Pasi A.; (439 pag.)WO2020/69106; (2020); A1;,
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