反应详情

温度

80 °C

A mixture of 5-cyclopropyl-1H-pyrazol-3-amine (415 mg, 3.37 mmol) and sodium (Z)-3-ethoxy-3-oxoprop-1-en-1-olate (0.791 g, 5.73 mmol) in EtOH (3 mL) and toluene (1 mL) was heated to 80° C. in a resealable tube. After 16 hrs the solvent was removed in vacuo. The resulting residue was dissolved in a minimal amount of warm water and triturated with 1 N HCl with cooling (0° C.) until the pH ˜1. The resulting solid was filtered and washed with water to afford 2-cyclopropylpyrazolo[1,5-a]pyrimidin-7-ol as an off-white solid that was advanced without further purification. M+H+ found=176.2.

1. customAfter 16 hrs the solvent was removed in vacuo
2. dissolutionThe resulting residue was dissolved in a minimal amount of warm water
3. customtriturated with 1 N HCl
4. temperaturewith cooling (0° C.) until the pH ˜1
5. filtrationThe resulting solid was filtered
6. washwashed with water