反应详情

温度

50 °C

Potassium tert-butoxide (1.0 M in THF, 0.7 mL, 0.7 mmol) was added to pyrrolidin-3-ylmethanol (0.06 g, 0.64 mmol) in THF (1.4 mL) and the mixture was stirred for 10 min at 50° C. 2-(6-Chloropyridazin-3-yl)-5-(1H-pyrazol-1-yl)phenol Intermediate 2-2 (0.05 g, 0.18 mmol) was added to the reaction at 0° C. and the mixture was stirred for 1 h at RT. Solvent was evaporated under reduced pressure. The crude material was purified via reverse phase preparative HPLC (5 to 95% acetonitrile in water, 5 mM NH4OH as modifier). Enantiomer 1 and Enantiomer 2 were isolated via preparative SFC. Two solids (11 mg (17%), and 12 mg (20%) were afforded.

1. stirringthe mixture was stirred for 1 h at RT
2. customSolvent was evaporated under reduced pressure
3. customThe crude material was purified via reverse phase preparative HPLC (5 to 95% acetonitrile in water, 5 mM NH4OH as modifier)
4. customEnantiomer 1 and Enantiomer 2 were isolated via preparative SFC
5. customTwo solids (11 mg (17%), and 12 mg (20%) were afforded