Reaktion #57652

Reaktionsgleichung

3-methyl-4-trifluoromethanesulfonyloxy-benzofuran-2-carboxylic acid tert-butyl ester

K3PO4

morpholine

dioxane

→

3-methyl-4-morpholin-4-yl-benzofuran-2-carboxylic acid tert-butyl ester

Ausbeute 60.5%

Lösungsmittel

water

Reaktionsbedingungen

Aufarbeitung

1. 1
   TemperaturThe mixture was heated
2. 2
   Extraktionwas extracted with ethyl acetate
3. 3
   ExtraktionThe organic extract
4. 4
   Waschenwas washed with water
5. 5
   Trocknendried over sodium sulfate
6. 6
   SonstigeRemoval of the solvent in vacuo
7. 7
   Sonstigegave the crude product, which
8. 8
   Sonstigewas purified by column chromatography

Vorschrift

To 3-methyl-4-trifluoromethanesulfonyloxy-benzofuran-2-carboxylic acid tert-butyl ester (190 mg, 0.5 mmol) was added K3PO4 (159 mg, 0.75 mmol), morpholine (52 mg, 0.6 mmol), Pd(OAc)2 (10 mg) and 4 mL of dioxane. The mixture was heated and stirred in an 85° C. oil bath overnight. The reaction mixture was poured into water and was extracted with ethyl acetate. The organic extract was washed with water and dried over sodium sulfate. Removal of the solvent in vacuo gave the crude product, which was purified by column chromatography to give 96 mg of 3-methyl-4-morpholin-4-yl-benzofuran-2-carboxylic acid tert-butyl ester, obtained as white solid.

Quelle