تفاعل #653199

ord-a66316c099734df8a182fadaba888a58

ظروف التفاعل

الظروف التفصيلية
See reaction.notes.procedure_details.

المعالجة

  1. 1
    درجة الحرارةthe mixture was refluxed for 16 hours
  2. 2
    غسيلThe organic layer was washed with saturated sodium chloride solution
  3. 3
    تجفيفdried with magnesium sulfate
  4. 4
    تركيزconcentrated under reduced pressure
  5. 5
    أخرىto give crude product (5.24 g)
  6. 6
    غسيلthe mixture was washed with ethyl acetate
  7. 7
    استخلاصthe mixture was extracted with ethyl acetate
  8. 8
    غسيلwashed with saturated sodium chloride solution
  9. 9
    تجفيفdried with magnesium sulfate
  10. 10
    تركيزconcentrated under reduced pressure

الإجراء التجريبي

Under argon atmosphere, a solution of methyl (E)-3-(5-bromothiophen-2-yl)acrylate (4.0 g), 4-methylphenyl borate (2.64 g) and potassium carbonate (4.48 g) in toluene-ethanol-water (160-16-16 ml) was stirred at room temperature for 1 hour. To the reaction mixture was added tetrakistriphenylphosphinepalladium (0.56 g), and the mixture was refluxed for 16 hours and cooled to room temperature. The organic layer was washed with saturated sodium chloride solution, dried with magnesium sulfate and concentrated under reduced pressure to give crude product (5.24 g). To a solution of the resulting carboxylic acid ester (5.24 g) in tetrahydrofuran (100 ml) was added 1N sodium hydroxide (20 ml) at room temperature, and the mixture was stirred for 5days. To the reaction mixture was added water, and the mixture was washed with ethyl acetate. The aqueous layer was acidified with concentrated hydrochloric acid, and the mixture was extracted with ethyl acetate, washed with saturated sodium chloride solution, dried with magnesium sulfate and concentrated under reduced pressure to give (E)-3-[5-(4-methylphenyl)-thiophen-2-yl]acrylic acid (1.9 g) as yellow crystals.

المصدر

DOI: 10.6084/m9.figshare.5104873.v1براءة الاختراع: US06172061B2uspto-grants-2001_01