Реакция #2298651

Уравнение реакции

H2O

3-(4-methyl-1-piperazinyl)-1-phenylsulfonyl-1H-indazole

K2CO3

cyanogen bromide

→

4-[1-(Phenylsulfonyl)-1H-indazol-3-yl]-1-piperazinecarbonitrile

Растворители

dimethylsulfoxide

DMSO

Условия реакции

Обработка

1. 1
   ДругоеThe solid, which precipitated from solution
2. 2
   Фильтрацияwas collected by filtration
3. 3
   Промывкаwas washed well with H2O affording 168 g (68%) of product
4. 4
   ДругоеA 5.2 g sample was recrystallized twice from ethanol-H2O yielding 4.0 g of 4-[1-(phenylsulfonyl)-1H-indazol-3-yl]-1-piperazinecarbonitrile, m.p.=178°-180° C.

Методика

To a stirred mixture of 3-(4-methyl-1-piperazinyl)-1-phenylsulfonyl-1H-indazole (237 g, 0.67 mol), K2CO3 (102 g, 0.74 mol) and dimethylsulfoxide (DMSO, 2000 ml), under nitrogen, was added cyanogen bromide (72 g, 0.68 mol) dissolved in DMSO (525 ml). The reaction was stirred at ambient temperature for 5.5 hours and was then poured into H2O (7 l). The solid, which precipitated from solution, was collected by filtration and was washed well with H2O affording 168 g (68%) of product. A 5.2 g sample was recrystallized twice from ethanol-H2O yielding 4.0 g of 4-[1-(phenylsulfonyl)-1H-indazol-3-yl]-1-piperazinecarbonitrile, m.p.=178°-180° C.

Источник