Реакция #57652

Уравнение реакции

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

Выход 60.5%

Растворители

water

Условия реакции

Обработка

1. 1
   ТемператураThe mixture was heated
2. 2
   Экстракцияwas extracted with ethyl acetate
3. 3
   ЭкстракцияThe organic extract
4. 4
   Промывкаwas washed with water
5. 5
   Сушкаdried over sodium sulfate
6. 6
   ДругоеRemoval of the solvent in vacuo
7. 7
   Другоеgave the crude product, which
8. 8
   Другоеwas purified by column chromatography

Методика

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.

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