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Dimethyl Sulfoxide → Methyl {1-[(2R)-2-{[(4-fluorophenyl)sulfonyl](methyl)amino}-4-oxobutyl]-1H-pyrrolo[2,3-b]pyridin-3-yl}acetate

HRID 1036637
Notizen
Druckvorschau

Reaktionsgleichung

Reaktionsgleichung von HRID 1036637
CS(C)=O.S(=O)(=O)=O.N1C=CC=CC=1.[F:15][C:16]1[CH:21]=[CH:20][C:19]([S:22]([N:25]([CH3:45])[C@H:26]([CH2:42][CH2:43][OH:44])[CH2:27][N:28]2[C:32]3=[N:33][CH:34]=[CH:35][CH:36]=[C:31]3[C:30]([CH2:37][C:38]([O:40][CH3:41])=[O:39])=[CH:29]2)(=[O:24])=[O:23])=[CH:18][CH:17]=1.CCN(C(C)C)C(C)C>ClCCl>[F:15][C:16]1[CH:21]=[CH:20][C:19]([S:22]([N:25]([CH3:45])[C@H:26]([CH2:42][CH:43]=[O:44])[CH2:27][N:28]2[C:32]3=[N:33][CH:34]=[CH:35][CH:36]=[C:31]3[C:30]([CH2:37][C:38]([O:40][CH3:41])=[O:39])=[CH:29]2)(=[O:24])=[O:23])=[CH:18][CH:17]=1
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Komponenten

6

Edukt 4

HCID 679Dimethyl SulfoxideHCID 81531DiisopropylethylamineHCID 168533Sulfur trioxide-pyridineHCID 86762092Methyl {1-[(2R)-2-{[(4-fluorophenyl)sulfonyl](methyl)amino}-4-hydroxybutyl]-1H-pyrrolo[2,3-b]pyridin-3-yl}acetate

Produkt 1

HCID 86762093Methyl {1-[(2R)-2-{[(4-fluorophenyl)sulfonyl](methyl)amino}-4-oxobutyl]-1H-pyrrolo[2,3-b]pyridin-3-yl}acetate

Reagenzien, Katalysatoren, Lösungsmittel 1

HCID 6344DichloromethaneLösungsmittel

Reaktionsbedingungen

Temperatur
-10 °C

Versuchsvorschrift

To DMSO (1 L, 1.41E+04 mmol) at room temperature was added pyridine sulfur trioxide (202.08 g, 1270 mmol) and the reaction mixture was stirred for 30 min at room temperature (solution A). In another flask, to a stirred solution of methyl {1-[(2R)-2-{[(4-fluorophenyl)sulfonyl](methyl)amino}-4-hydroxybutyl]-1H-pyrrolo[2,3-b]pyridin-3-yl}acetate (273 g, 589 mmol) and Hunig's base (0.425 L, 2433 mmol) in dichloromethane (4 L) at −10° C. was added solution A dropwise over 30 min. The reaction was stirred at −10° C. for 1 h. then quenched by adding ½ saturated brine (4 L); the aqueous layer was neutralized with solid sodium bicarbonate. The layers were then separated and the organic layer was washed with ½ saturated brine (4 L), dried over sodium sulfate, filtered and evaporated under reduced pressure. The residue was purified by flash chromatography with ethyl acetate to provide the title compound.

Aufarbeitung

  1. customthen quenched
  2. additionby adding ½ saturated brine (4 L)
  3. customThe layers were then separated
  4. washthe organic layer was washed with ½ saturated brine (4 L)
  5. dry with materialdried over sodium sulfate
  6. filtrationfiltered
  7. customevaporated under reduced pressure
  8. customThe residue was purified by flash chromatography with ethyl acetate

Quellen und Nachweise

ORD-Eintrag
ord-7412807aa60847c3b55ee29bd92de4e2
Quelldatensatz
uspto-grants-2013_10
DOI
10.6084/m9.figshare.5104873.v1
Patentnummer
US08546422B2

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