HRID1400717

反应详情

EQUATION

反应方程式

HRID 1400717 的结构方程式

AUXILIARIES

试剂、催化剂与溶剂

2

CONDITIONS

反应条件

温度
80 °C

PROCEDURE

实验过程

A solution of (2S)-methyl 2-(7-(4-allylchroman-6-yl)-2-(2′-(allyloxy)-[1,1′-biphenyl]-3-yl)-5-methylpyrazolo[1,5-a]pyrimidin-6-yl)-2-(tert-butoxy)acetate (0.373 g, 0.567 mmol) in DCE (275 ml) was heated (70° C.) and then treated with Hoveyda-Grubbs cat.2nd gen. (0.025 g, 0.040 mmol). The reaction was stirred for 2.5 hrs, then additional catalyst (0.025 g, 0.040 mmol) was added, the temperature was raised (80° C.) and the reaction was stirred for 30 min. The reaction was cooled, concentrated, and the residue was purified by biotage (24 g SiO2, 0% (3 CV), 0-60% (15 CV), 60% (2 CV), EtOAc in hexanes) to afford the desired product (0.300 g, 0.476 mmol, 84% yield). LCMS (M+H)=630.5.

WORKUP

后处理

  1. stirringthe reaction was stirred for 30 min
  2. temperatureThe reaction was cooled
  3. concentrationconcentrated
  4. customthe residue was purified by biotage (24 g SiO2, 0% (3 CV), 0-60% (15 CV), 60% (2 CV), EtOAc in hexanes)