HRID1670820

反应详情

EQUATION

反应方程式

HRID 1670820 的结构方程式

AUXILIARIES

试剂、催化剂与溶剂

4

CONDITIONS

反应条件

温度
80 °C

PROCEDURE

实验过程

Bring a mixture of trifluoro-methanesulfonic acid 4-{3-[4-(tert-butyl-diphenyl-silanyloxy)-cyclohexyl]-2-oxo-pyrrolidin-1-ylmethyl}-3,5-dichloro-phenyl ester (0.61 g, 0.84 mmol), 4-methoxycarbonylphenylboronic acid (0.18 g, 1 mmol), sodium carbonate (0.267 g, 2.52 mmol) in THF (15 mL) and water (5 mL) to 60° C. To the mixture at 60° C., add Pd(PPh3)4 (0.048 g, 0.04 mmol). Raise the reaction temperature to 80° C. and stir for 1 hour. Cool the reaction, dilute with ethyl acetate, and wash with water and brine. Dry the organic layer (Na2SO4), remove the solvent in vacuo to afford crude product, and purify on silica gel column with 25% ethyl acetate in hexanes to afford 0.56 g (93%) of the titled product. MS (m/z): 714 (M+).

WORKUP

后处理

  1. temperatureCool
  2. customthe reaction
  3. washwash with water and brine
  4. dry with materialDry the organic layer (Na2SO4)
  5. customremove the solvent in vacuo
  6. customto afford crude product
  7. custompurify on silica gel column with 25% ethyl acetate in hexanes