반응 #90510

ord-967c8d0010d84551a695b32202a2ba3e

용매

반응 조건

상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    온도The mixture was cooled in an ice bath
  2. 2
    기타at room temperature
  3. 3
    기타overnight
  4. 4
    추출the mixture was extracted with ethyl acetate twice
  5. 5
    세척The combined organic layers were washed with water and brine
  6. 6
    건조dried over anhydrous sodium sulfate
  7. 7
    농축concentrated
  8. 8
    기타The crude was purified first by flash chromatography

실험 절차

To a 100 mL round bottom flask were added dibenzyl (chloromethyl) phosphate (1.632 g, 4.99 mmol), (S)-benzyl 2-benzyl-2-(1-(benzyloxy)-3-(3-(benzyloxy)-4-hydroxyphenyl)-2-methyl-1-oxopropan-2-yl)hydrazinecarboxylate, Compound 2, (2.1 g, 3.33 mmol) and 25 mL acetonitrile. The mixture was cooled in an ice bath. 1,8-Diazabicyclo[5.4.0]undec-7-ene (0.745 mL, 4.99 mmol) was added, and the mixture was stirred in the ice bath for 30 minutes, then at room temperature overnight. Water was added to the reaction mixture, and the mixture was extracted with ethyl acetate twice. The combined organic layers were washed with water and brine, dried over anhydrous sodium sulfate, and concentrated. The crude was purified first by flash chromatography using a 120 g silica column (0-50% ethyl acetate in heptanes), followed by RP-HPLC (60-100% acetonitrile in 0.1% TFA/water on Phenonemex C18 5 u column) to afford Compound 3 as a colorless oil (247 mg, 8%).

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US09446059B2uspto-grants-2016_09