反応 #50919

反応方程式

sodium carbonate

405

tert-Butyl 2-(3-cyanophenyl)-3-(4-iodophenylaminocarbonyl)-3-propylcarbazate

2-(methylthio)-phenylboronic acid

→

409

収率 85.9%

tert-Butyl 2-(3-cyanophenyl)-3-(2′-methylthiobiphenyl-4-ylaminocarbonyl)-3-propylcarbazate

収率 85.9%

溶媒

ethylene glycol dimethyl ether

反応条件

実験手順

1.5 g (2.883 mmol) of 405 and 0.968 g (5.766 mmol) of 2-(methylthio)-phenylboronic acid are dissolved in 100 ml of ethylene glycol dimethyl ether, treated with 63 mg (0.086 mmol) of PdCl2(dppf) and 20.0 ml of 2N sodium carbonate solution and then stirred at 110° C. under a nitrogen atmosphere for 3 h. After customary work-up, 1.28 g (75.9%) of 409 are thus obtained as crystals having a melting point of 184-185° C.; MS(FAB)=517.

出典