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877399-60-5

4-(4-Bromo-pyrazol-1-yl)-piperidine synthesis

5synthesis methods
-

Yield:877399-60-5 96.6%

Reaction Conditions:

with trifluoroacetic acid in dichloromethane at 0 - 20; for 16 h;

Steps:

1.4 Step 4:

In a 500 mL single-neck flask, 6 (9.8 g, 35.8 mmol) was dissolved in DCM (80 mL), TFA (16 mL) was added dropwise at 0°C, and the reaction was carried out at room temperature for 16 h. Concentrate at low temperature, add DCM (200 mL) to dilute, add ice water to quench, adjust pH=10 with ammonia water at 0 °C, extract with DCM (200 mL×3), wash the organic phase with saturated brine (200 mL×2), dry It was dried over sodium sulfate and spin-dried to obtain 6.59 g of the target product as a white solid (yield: 96.6%).

References:

CN114767676,2022,A Location in patent:Paragraph 0268-0269; 0280-0282