反应详情

温度

45 °C

Tert-butyl-N-(5-amino-6-bromopyridin-2-yl)carbamate A5 (617 mg, 1.82 mmol), ethynylbenzene (420 μl, 3.82 mmol), copper(I) iodide (35 mg, 0.18 mmol), 1,1′-Bis-(diphenylphosphino)ferrocene]dichloropalladium(II) (66.4 mg, 0.09 mmol) and triethylamine (631 μl, 4.55 mmol) are stirred under argon atmosphere in a mixture of ACN (10 ml) and THF (5 ml) for 2 h at RT. The mixture is warmed to 45° C. and stirred for 70 h. The mixture is concentrated in vacuo and the product purified by RP HPLC. Yield: 320 mg (57%). HPLC-MS: M+H=310; tR=2.05 min (*Method—2).

1. concentrationThe mixture is concentrated in vacuo
2. customthe product purified by RP HPLC