Реакция #602

ord-1e9ec853eb3e43adb71af85c977827e9

Уравнение реакции

Brc1ccc(Br)cc1
Brc1ccc(Br)cc1
CC1CNC1
CC1CNC1
CC1CN(c2ccc(Br)cc2)C1
CC1CN(c2ccc(Br)cc2)C
Выход 84.7%

Растворители

Условия реакции

Температура
100°CELSIUS

Методика

3-methylazetidine (0.5 g, 4.69 mmol), diacetoxypalladium (10.53 mg, 0.05 mmol), 2,2'-bis(diphenylphosphino)-1,1'-binaphthyl (0.058 g, 0.09 mmol) and cesium carbonate (3.67 g, 11.26 mmol), degassed toluene (15 mL) were heated at 100 °C over the weekend. The RM was filtered and washed with EtOAc the filtrate was then concentrated and the crude product purified by flash silica chromatography, elution gradient 20 to 30% EtOAc in heptane. Purest fractions were collected and combined with EN05604-93. The combined product was then recrystalised from EtOAc to give 1-(4-bromophenyl)-3-methylazetidine (0.899 g, 85 %).

Источник

750 AstraZeneca ELN dataset