반응 #69618

ord-614784044f794cf8b0eff799eaebc3ac

반응 방정식

CC(C)(C)c1cccc(C=O)c1O
3-tert-butyl-2-hydroxybenzaldehyde
COc1ccc(CCl)cc1
4-methoxybenzyl chloride
O=C([O-])[O-].[K+].[K+]
K2CO3
CC#N
MeCN
COc1ccc(COc2c(C=O)cccc2C(C)(C)C)cc1
24
수율 89.5%
COc1ccc(COc2c(C=O)cccc2C(C)(C)C)cc1
3-tert-Butyl-2-(4-methoxybenzyloxy)benzaldehyde
수율 89.5%

반응 조건

상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    온도was refluxed for 6 hr
  2. 2
    기타for 48 hr
  3. 3
    여과filtered
  4. 4
    세척washing the solids with EtOAc (50 mL)
  5. 5
    농축The filtrate was concentrated under reduced pressure
  6. 6
    기타to give brown oil
  7. 7
    세척the solution washed with H2O (125 mL) and brine (100 mL)
  8. 8
    건조The organic phase was dried over Na2SO4
  9. 9
    여과filtered
  10. 10
    농축the solution concentrated under reduced pressure
  11. 11
    기타to give a brown oil
  12. 12
    기타The crude product was absorbed onto silica gel
  13. 13
    세척The column was eluted with heptanes (500 mL)
  14. 14
    농축Product fractions were concentrated under reduced pressure
  15. 15
    기타to give a yellow oil
  16. 16
    기타crystallization
  17. 17
    기타After crystallization

실험 절차

A suspension of 3-tert-butyl-2-hydroxybenzaldehyde (5.0 g, 28.1 mmol, 1.0 equiv), 4-methoxybenzyl chloride (4.4 g, 3.8 mL, 28.1 mmol, 1.0 equiv), powdered K2CO3 (7.8 g, 56.2 mmol, 2.0 equiv) and MeCN (100 mL) was refluxed for 6 hr. The yellow-green suspension was cooled to room temperature and allowed the stand for 48 hr. The suspension was diluted with EtOAc (50 mL) and filtered, washing the solids with EtOAc (50 mL). The filtrate was concentrated under reduced pressure to give brown oil. The oil was dissolved in EtOAc (150 mL) and the solution washed with H2O (125 mL) and brine (100 mL). The organic phase was dried over Na2SO4, filtered and the solution concentrated under reduced pressure to give a brown oil. The crude product was absorbed onto silica gel using dichloromethane and dry-loaded onto a column of silica gel (100 g) packed in heptanes. The column was eluted with heptanes (500 mL) followed by 2.5% EtOAc/heptanes (1000 mL). Product fractions were concentrated under reduced pressure to give a yellow oil. Seeding (seeds obtained by lengthy scratching with cold hexanes) of the oil induced crystallization. After crystallization was complete the yellow solid was pumped under high vacuum for 0.5 hr to give 7.5 g (89%) of 24.

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US08530593B2uspto-grants-2013_09