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Sodium hydride → 2-(5-Chloro-indolin-1-yl)benzamide

HRID 3990
Notizen
Druckvorschau

Reaktionsgleichung

Reaktionsgleichung von HRID 3990
[Cl:1][C:2]1[CH:3]=[C:4]2[C:8](=[CH:9][CH:10]=1)[NH:7][CH2:6][CH2:5]2.[H-].[Na+].F[C:14]1[CH:22]=[CH:21][CH:20]=[CH:19][C:15]=1[C:16]([NH2:18])=[O:17]>CS(C)=O>[Cl:1][C:2]1[CH:3]=[C:4]2[C:8](=[CH:9][CH:10]=1)[N:7]([C:14]1[CH:22]=[CH:21][CH:20]=[CH:19][C:15]=1[C:16]([NH2:18])=[O:17])[CH2:6][CH2:5]2
KomponentenVersuchsvorschriftAufarbeitungQuellen und NachweiseNotizen zur Reaktion

Komponenten

5

Edukt 3

HCID 24758Sodium hydrideHCID 679642-FluorobenzamideHCID 1175965-Chloroindoline

Produkt 1

HCID 138233482-(5-Chloro-indolin-1-yl)benzamideAusbeute 43,3 %

Reagenzien, Katalysatoren, Lösungsmittel 1

HCID 679Dimethyl SulfoxideLösungsmittel2×

Versuchsvorschrift

A slurry was prepared comprising 5-chloroindoline (15.3 gm, 0.1 mole), dimethylsulfoxide (DMSO) [50 ml] and sodium hydride (5.28 gm, 50% in oil, washed with hexane). The slurry was permitted to stir at room temperature for 1 hour. To this a solution of o-fluorobenzamide (15.2 gm, 1.1 eq.) in DMSO (20 ml) was added dropwise with the temperature between 17°-19° C. At the end of addition the reaction mixture was stirred at room temperature for 2 hours, then heated to 75°-78° C. for 16 hours. The reaction mixture was partitioned between methylene chloride (300 ml) and water (250 ml). The aqueous phase was separated and extracted twice with methylene chloride (150 ml). The combined organic solution was washed twice with water, twice with HCl (2N, 100 ml), brine (2×50 ml), dried over Na2SO4, concentrated to about 50 ml. Ether (50 ml) was added. The product was crystallized out upon standing overnight (about 16 hours). The yield was 14.2 gm (52%); m.p. 137°-138° C. Recrystallization from methylene chloride and ether yielded 2-(5-chloro-indolin-1-yl)benzamide (11.82 gm) m.p. 137°-138° C.

Aufarbeitung

  1. additionAt the end of addition the reaction mixture
  2. stirringwas stirred at room temperature for 2 hours
  3. temperatureheated to 75°-78° C. for 16 hours
  4. customThe reaction mixture was partitioned between methylene chloride (300 ml) and water (250 ml)
  5. customThe aqueous phase was separated
  6. extractionextracted twice with methylene chloride (150 ml)
  7. washThe combined organic solution was washed twice with water, twice with HCl (2N, 100 ml), brine (2×50 ml)
  8. dry with materialdried over Na2SO4
  9. concentrationconcentrated to about 50 ml
  10. additionEther (50 ml) was added
  11. customThe product was crystallized out
  12. waitupon standing overnight
  13. custom(about 16 hours)
  14. customRecrystallization from methylene chloride and ether

Quellen und Nachweise

ORD-Eintrag
ord-34a0944dc3144a9f9ca25f89152134d8
Quelldatensatz
uspto-grants-1988_02
DOI
10.6084/m9.figshare.5104873.v1
Patentnummer
US04723007

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