반응 #590863

ord-ff978230dfc34c4180f71245d4f60ce8

용매

반응 조건

상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    추출after a further 30 min the aqueous phase was extracted with CH2Cl2 (2×70 mL)
  2. 2
    기타the combined organic phase were dried
  3. 3
    농축concentrated under reduced pressure
  4. 4
    기타the residue was purified by column chromatography on silica gel
  5. 5
    세척Elution with EtOAc/petroleum ether (1:1 to 1:0)

실험 절차

A solution of methyl 3-[bis(2-hydroxyethyl)amino]-2,6-dinitrobenzoate [Palmer et al., J. Med. Chem. 1996, 39, 2518] (7.24 g, 22 mmol) in CH2Cl2 (120 mL) was cooled in an ice-bath and Et3N (15 mL) and MsCl (8 mL) were added in one portion. After stirred for 10 min, satd. NaHCO3 (100 mL) was added, and after a further 30 min the aqueous phase was extracted with CH2Cl2 (2×70 mL), the combined organic phase were dried, concentrated under reduced pressure, and the residue was purified by column chromatography on silica gel. Elution with EtOAc/petroleum ether (1:1 to 1:0), gave crude methyl 3-(bis{2-[(methylsulfonyl)oxy]ethyl}amino)-2,6-dinitrobenzoate (16) (10.67 g, 100%) as a yellow oil;

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US07776924B2uspto-grants-2010_08