反应 #637128

ord-eb59adcd898b47b4a81f9cc68aa5b946

溶剂

反应条件

详细条件
See reaction.notes.procedure_details.

后处理

  1. 1
    萃取After aqueous work-up, the mixture is extracted with ethyl acetate
  2. 2
    干燥the extracts are dried with sodium sulphate
  3. 3
    浓缩concentrated under reduced pressure
  4. 4
    其他The residue is purified chromatographically

实验过程

Under argon, tert-butyl 4-(4-formyl-1,3-thiazol-2-yl)piperidine-1-carboxylate (600 mg) is dissolved in methanol, and potassium carbonate (839 mg) and dimethyl 1-diazo-2-oxopropylphosphonate (786 mg) are added. The mixture is stirred at room temperature for 3 hours. After aqueous work-up, the mixture is extracted with ethyl acetate and the extracts are dried with sodium sulphate and concentrated under reduced pressure. The residue is purified chromatographically. This gives tert-butyl 4-(4-ethynyl-1,3-thiazol-2-yl)piperidine-1-carboxylate (493 mg).

来源

DOI: 10.6084/m9.figshare.5104873.v1专利: US07943774B2uspto-grants-2011_05