반응 #472841

ord-409ad538074b4ad0ad1c5dd313fa88ad

반응 방정식

O=C([O-])O.[Na+]
sodium hydrogen carbonate
O=CCn1c(=O)ccc2ncc(-n3ccnc3)cc21
(7-(1H-imidazol-1-yl)-2-oxo-1,5-naphthyridin-1(2H)-yl)acetaldehyde
CC(C)(C)OC(=O)N(Cc1cc2c(cn1)OCCO2)C1CCNCC1
tert-butyl (2,3-dihydro(1,4)dioxino(2,3-c)pyridin-7-ylmethyl)(piperidin-4-yl)carbamate
CC(=O)O[BH-](OC(C)=O)OC(C)=O.[Na+]
sodium triacetoxyborohydride
CC(C)(C)OC(=O)N(Cc1cc2c(cn1)OCCO2)C1CCN(CCn2c(=O)ccc3ncc(-n4ccnc4)cc32)CC1
tert-butyl (2,3-dihydro(1,4)dioxino(2,3-c)pyridin-7-ylmethyl)(1-(2-(7-(1H-imidazol-1-yl)-2-oxo-1,5-naphthyridin-1(2H)-yl)ethyl)piperidin-4-yl)carbamate
수율 51.0%

반응 조건

상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    기타the organic layer was separated
  2. 2
    추출the aqueous layer was extracted with chloroform
  3. 3
    세척the resultant solution was washed with water
  4. 4
    건조a saturated aqueous sodium chloride solution and dried over anhydrous magnesium sulfate
  5. 5
    workup.DISTILLATIONthe solvent was distilled off under reduced pressure
  6. 6
    기타The resultant residue was purified by basic silica gel column chromatography
  7. 7
    세척elution with chloroform

실험 절차

To a solution of 0.12 g of (7-(1H-imidazol-1-yl)-2-oxo-1,5-naphthyridin-1(2H)-yl)acetaldehyde in 1 mL of dichloromethane, a solution of 0.14 g of tert-butyl (2,3-dihydro(1,4)dioxino(2,3-c)pyridin-7-ylmethyl)(piperidin-4-yl)carbamate in 1.4 mL of dichloromethane, and 23 μL of acetic acid and 0.13 g of sodium triacetoxyborohydride were added, and the mixture was stirred at room temperature for 1 hour 40 minutes. The reaction mixture was charged with chloroform, and a saturated aqueous sodium hydrogen carbonate solution and adjusted to pH 8.6, the organic layer was separated and the aqueous layer was extracted with chloroform. The organic layer and the extract were combined, the resultant solution was washed with water and a saturated aqueous sodium chloride solution and dried over anhydrous magnesium sulfate, and the solvent was distilled off under reduced pressure. The resultant residue was purified by basic silica gel column chromatography using gradient elution with chloroform:methanol=19:1 to 93:7 to obtain 0.12 g of tert-butyl (2,3-dihydro(1,4)dioxino(2,3-c)pyridin-7-ylmethyl)(1-(2-(7-(1H-imidazol-1-yl)-2-oxo-1,5-naphthyridin-1(2H)-yl)ethyl)piperidin-4-yl)carbamate as a light yellow solid.

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US08367831B2uspto-grants-2013_02