Water → HCID 71515595, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of 1-[3-(3-trifluoromethoxy-phenyl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-ethanone (3e) (0.461 mmol), 0.44 g, 2.65 mmol), (1aS,6aR)-3,5-difluoro-6,6a-dihydro-1aH-1-oxa-cyclopropa[a]indene (6b) (0.077 g, 0.461 mmol) and K2CO3 (127 mg, 0.922 mmol) in 5 ml CH3CN was stirred at 50° C. for 24 h. Water was added, the mixture was extracted 3 times with CH2Cl2, the combined organic layers were dried over MgSO4, filtrated and the solution was evaporated to dryness. The crude product was purified by reverse phase HPLC (CH3CN/water gradient with 0.1% trifluoroacetic acid) to give 53 mg of 1-[1-((1R,2R)-4,6-difluoro-2-hydroxy-indan-1-yl)-3-(3-trifluoromethoxy-phenyl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-5-yl]-ethanone (11a).

Provenance & Evidence