Reaktion #472839

ord-90761071a0074fbab3149d07663afabb

Reaktionsgleichung

COc1cnc2ccc(=O)n(CC=O)c2n1
(3-methoxy-6-oxopyrido(2,3-b)pyrazin-5(6H)-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
O=C([O-])O.[Na+]
sodium hydrogen carbonate
COc1cnc2ccc(=O)n(CCN3CCC(N(Cc4cc5c(cn4)OCCO5)C(=O)OC(C)(C)C)CC3)c2n1
tert-butyl (2,3-dihydro(1,4)dioxino(2,3-c)pyridin-7-ylmethyl)(1-(2-(3-methoxy-6-oxopyrido(2,3-b)pyrazin-5(6H)-yl)ethyl)piperidin-4-yl)carbamate
Ausbeute 112.4%

Reaktionsbedingungen

Detaillierte Bedingungen
See reaction.notes.procedure_details.

Aufarbeitung

  1. 1
    Sonstigethe organic layer was separated
  2. 2
    Extraktionthe aqueous layer was extracted with chloroform
  3. 3
    Waschenthe resultant solution was washed with a saturated aqueous sodium chloride solution
  4. 4
    Trocknendried over anhydrous magnesium sulfate
  5. 5
    workup.DISTILLATIONthe solvent was distilled off under reduced pressure
  6. 6
    SonstigeThe resultant residue was purified by silica gel column chromatography

Vorschrift

To a solution of 0.12 g of (3-methoxy-6-oxopyrido(2,3-b)pyrazin-5(6H)-yl)acetaldehyde in 5 mL of methylene chloride, 0.18 g of tert-butyl (2,3-dihydro(1,4)dioxino(2,3-c)pyridin-7-ylmethyl)(piperidin-4-yl)carbamate, 26 μL of acetic acid and 0.12 g of sodium triacetoxyborohydride were added, and the mixture was stirred at room temperature for 2 hours 30 minutes. To the reaction mixture, a saturated aqueous sodium hydrogen carbonate solution and chloroform were added, 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 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 silica gel column chromatography using an eluent of chloroform:methanol=20:1 to obtain 0.32 g of tert-butyl (2,3-dihydro(1,4)dioxino(2,3-c)pyridin-7-ylmethyl)(1-(2-(3-methoxy-6-oxopyrido(2,3-b)pyrazin-5(6H)-yl)ethyl)piperidin-4-yl)carbamate as a colorless oily substance.

Quelle

DOI: 10.6084/m9.figshare.5104873.v1Patent: US08367831B2uspto-grants-2013_02