反应详情

A suspension of 91.35 g (0.225 mol) of 2-[3-(4-bromo-2,5-difluorophenyl)cyclopentyl]-1H-isoindole-1,3-(2H)-dione, 22.4 g (0.25 mol) of copper (I) cyanide and 250 ml of N,N-dimethylformamide was stirred and heated in a nitrogen atmosphere at 170° for 18 hours. The cooled mixture was poured into a solution of 100 ml of concentrated ammonium hydroxide in 1 L of water. The aqueous mixture was extracted with ether (4×350 ml) and the combined ether layers were washed with water (3×300 ml), dried (MgSO4), and evaporated in vacuo to give 71.2 g of the title compound which was used as is for the next step.

1. temperatureheated in a nitrogen atmosphere at 170° for 18 hours
2. extractionThe aqueous mixture was extracted with ether (4×350 ml)
3. washthe combined ether layers were washed with water (3×300 ml)
4. dry with materialdried (MgSO4)
5. customevaporated in vacuo