反应 #170241

ord-99f898b4185b45aaabdee714fe8b2e5d

反应条件

详细条件
See reaction.notes.procedure_details.

后处理

  1. 1
    萃取extracted with dichloromethane (3×50 mL)
  2. 2
    干燥The combined organic layers were dried over sodium sulfate
  3. 3
    过滤filtered
  4. 4
    浓缩concentrated to dryness

实验过程

To a solution of 1-benzhydryl-3-(benzofuran-3-yl)azetidin-3-ol (760 mg, 2.14 mmol) in dichloromethane (10 mL) was added at 0° C. triethylamine (387 μL, 2.78 mmol) and then dropwise a solution of methanesulfonyl chloride (216 μL, 2.78 mmol) in dichloromethane (3 mL). The reaction mixture was stirred for 1 hour at room temperature, then diluted with water (50 mL) and extracted with dichloromethane (3×50 mL). The combined organic layers were dried over sodium sulfate, filtered and concentrated to dryness. The crude title compound was obtained as a yellow gum (873 mg, 109%) and used for the next step without further purification.

来源

DOI: 10.6084/m9.figshare.5104873.v1专利: US08846711B2uspto-grants-2014_09