Triethyloxonium tetrafluoroborate → 1H-PYRAZOLO[3,4-C]PYRIDINE, 1-CYCLOPENTYL-7-ETHOXY-3-ETHYL-4,5-DIHYDRO-

Participants

Reaction Steps

A solution of triethyloxonium tetrafluoroborate (3.371 kg, 17.74 moles) in methylene chloride (10.8 L) was slowly added to a suspension of 1-cyclopentyl-3-ethyl-1,4,5,6-tetrahydro-pyrazolo[3,4-c]pyridin-7-one (3.6 kg, 15.43 moles) in methylene chloride (7.2 L) over a period of about 40 minutes. The solution was then allowed to react for about 21 hours at 18-22° C. After the reaction was complete, the organic solution was washed with aqueous 10 % sodium carbonate (36 L) and evaporated to an oil which was used directly in the next step. The yield for this step was 92.9%.

Provenance & Evidence