These common heterocyclic compound, 1260243-04-6, name is Ethyl 5-amino-1H-pyrazole-4-carboxylate, its 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. Recommanded Product: 1260243-04-6
To a mixture of ethyl 5-amino- lH-pyrazole-4-carboxylate (150.00 g, 1.08 mmol) and ethyl (E)-3-ethoxyprop-2-enoate (292.16 g, 2.03 mol) in DMF (3.2 L) was added Cs2C03 (656.77 g, 2.02 mol) in one portion at 20 °C under N2. The mixture was stirred at 110 °C for 6 h. TLC (PE: EtOAc=l : 1) showed the reaction was completed. The mixture was cooled to 20 °C and filtered through a celite pad. The filter cake was washed with ethyl acetate (3X30 mL). The filtrate was added to H20 (2 L) and acidified with HOAc to pH=4. The resultant precipitate was filtered to afford A-1-7 (173.00 g, 834.98 mmol, 86.36percent yield) as a white solid: 1H NMR (400 MHz, DMSO-d6) delta 8.54 (d, 7=7.91 Hz, 1H), 8.12 (s, 1H), 6.13 (d, 7=7.91 Hz, 1H), 4.27 (q, 7=7.11 Hz, 2H), 1.28 (t, 7=7.09 Hz, 3H).
The synthetic route of Ethyl 5-amino-1H-pyrazole-4-carboxylate has been constantly updated, and we look forward to future research findings.
Reference:
Patent; TP THERAPEUTICS, INC.; CUI, Jingrong J.; LI, Yishan; ROGERS, Evan W.; ZHAI, Dayong; DENG, Wei; UNG, Jane; (170 pag.)WO2017/4342; (2017); A1;,
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