반응 #320311

ord-9bf37336c2944d3d8f504448f0d028b1

반응 조건

온도
0°CELSIUS
상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    온도slowly warmed
  2. 2
    온도heated
  3. 3
    온도The solution was cooled to 70° C.
  4. 4
    workup.STIRRINGThe mixture was then stirred at 70° C. for 90 minutes
  5. 5
    온도after cooling
  6. 6
    기타the organic phase was separated off
  7. 7
    추출extracted
  8. 8
    workup.STIRRINGby shaking with 100 ml of water
  9. 9
    농축concentrated
  10. 10
    기타An organic phase was obtained from the aqueous mother liquor by extraction with methylene chloride and concentration

실험 절차

33.8 g of aluminium chloride were suspended in 200 g of fluorobenzene, and a solution of 37.8 g of thiophene-2-carbonyl chloride in 50 ml of fluorobenzene was added dropwise to this at 0° C. over the course of 30 minutes. The mixture was stirred at 0° C. for 2 hours and then slowly warmed, and heated under reflux at 85° C. for 2 hours until evolution of hydrogen chloride ceased. The solution was cooled to 70° C. and then, at this temperature, added dropwise over the course of 30 minutes to a stirred suspension of 7.2 g of of sodium borohydride in 50 ml of diglyme. The mixture was then stirred at 70° C. for 90 minutes and, after cooling, discharged into a mixture of 250 g of ice, 200 ml of water and 62.5 g of concentrated aqueous hydrochloric acid. After addition of 100 ml of fluorobenzene, the organic phase was separated off, extracted by shaking with 100 ml of water and concentrated. Yield: 58.3 g of product with a content of 61.8% by weight of 2-(4-fluorobenzyl)thiophene (GC), corresponding to a yield of 75.1% of theory. An organic phase was obtained from the aqueous mother liquor by extraction with methylene chloride and concentration and contained a further 33.7% by weight of the required product (GC), corresponding to an additional yield of 4.6% of theory. Distillation of the organic phase resulted in a 99.2% pure 2-(4-fluorobenzyl)thiophene.

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US05591869uspto-grants-1997_01