تفاعل #9000

ord-7ef5756414e1483ebd37c8a4117aa494

ظروف التفاعل

الظروف التفصيلية
See reaction.notes.procedure_details.

المعالجة

  1. 1
    غسيلwashed with brine (3×15 mL)
  2. 2
    تجفيفdried (Na2SO4)
  3. 3
    تركيزconcentrated
  4. 4
    أخرىto provide a pale yellow solid
  5. 5
    درجة الحرارةheated at 80° C. overnight
  6. 6
    درجة الحرارةThe mixture was cooled to room temperature
  7. 7
    أخرىThe phases were separated
  8. 8
    غسيلthe organic phase was washed with 1.0 N NaOH (6×10 mL) and brine (2×20 mL)
  9. 9
    تجفيفThe organic phase was dried (MgSO4)
  10. 10
    تركيزconcentrated
  11. 11
    أخرىto provide an pale yellow solid
  12. 12
    غسيلThe solid was rinsed with hexanes (3×10 mL)

الإجراء التجريبي

To a solution of 2-methoxy-6-methylbenzyl alcohol (0.96 g, 6.32 mmol) in CH2Cl2 (35 mL) was added triethylamine (2.00 mL, 14.35 mmol) followed by methanesulfonyl chloride (0.90 mL, 11.63 mmol) and the resultant solution was heated at 40° C. for 45 minutes then cooled to room temperature. The mixture was diluted with CH2Cl2 (35 mL), washed with brine (3×15 mL), dried (Na2SO4), and concentrated to provide a pale yellow solid. The solid (1.12 g) was dissolved in DMF (35 mL), treated with potassium phthalimide (2.62 g, 14.15 mmol), and heated at 80° C. overnight. The mixture was cooled to room temperature and diluted with EtOAc (70 mL), brine (35 mL), and water (20 mL). The phases were separated and the organic phase was washed with 1.0 N NaOH (6×10 mL) and brine (2×20 mL). The organic phase was dried (MgSO4) and concentrated to provide an pale yellow solid. The solid was rinsed with hexanes (3×10 mL) and provided 1.18 g (66%) of (2-methoxy-6-methylbenzyl)phthalimide as a white solid. 1H NMR (CDCl3) δ 2.53 (s, 3H), 3.75 (s, 3H), 4.89 (s, 2H), 6.70 (d, 1H, J=8.4 Hz), 6.80 (d, 1H, J=7.5 Hz), 7.15 (dd, 1H, J=7.5, 8.4 Hz), 7.66–7.68 (m, 2H), 7.76–7.80 (m, 2H); 13C NMR (CDCl3) δ 20.27, 34.95, 55.90, 108.61, 122.38, 123.17, 123.41, 128.97, 132.60, 134.07, 139.55, 158.70, 168.36.

المصدر

DOI: 10.6084/m9.figshare.5104873.v1براءة الاختراع: US07091217B2uspto-grants-2006_08