反应详情

This compound was prepared from (±) 3-cyano-1-azabicyclo[2.2.2]octane (EP-A-0 261 763, Description 1) in a similar manner to the compound of Example 2 using an ethereal solution of diazoethane prepared from N-nitroso-N-ethyl urea1,2. The resulting oil was purified by column chromatography using neutral alumina and eluting with 2% MeOH/EtOAc. 1H NMR indicated that the mixture contained a 12:1 ratio of the 2-ethyl isomer to 1-ethyl isomer and this mixture (100 mg, 17%) was crystallised and the title compound E9 recrystallised from methanol/diethyl ether as the oxalate salt (containing 8% of the 1-ethyl isomer).

1. customprepared from N-nitroso-N-ethyl urea1,2
2. customThe resulting oil was purified by column chromatography
3. washeluting with 2% MeOH/EtOAc
4. customthis mixture (100 mg, 17%) was crystallised
5. customthe title compound E9 recrystallised from methanol/diethyl ether as the oxalate salt (containing 8% of the 1-ethyl isomer)