Реакция #74277

Уравнение реакции

(1-benzyl-4-(4-cyclopropylpiperazin-1-yl)piperidin-4-yl)methanamine

methyl 2-(bromomethyl)benzoate

triethylamine

→

crude product

Выход 51.0%

2-((1-Benzyl-4-(4-cyclopropylpiperazin-1-yl)piperidin-4-yl)methyl)-isoindolin-1-one

Выход 51.0%

Растворители

benzene

Условия реакции

Обработка

1. 1
   Другоеthe resulting reaction mixture
2. 2
   Температураwas refluxed for 25 h
3. 3
   Другоеthe solvent was evaporated under reduced pressure
4. 4
   workup.DISSOLUTIONThe residue was dissolved in ethyl acetate
5. 5
   Промывкаthe organic layer was successively washed with water and brine
6. 6
   СушкаThe organic layer was dried over sodium sulfate
7. 7
   Другоеthe solvent was evaporated under reduced pressure

Методика

To a solution of (1-benzyl-4-(4-cyclopropylpiperazin-1-yl)piperidin-4-yl)methanamine (see above: synthesis of amine AM12) (1.22 mmol, 1.0 equiv.) and methyl 2-(bromomethyl)benzoate (1.22 mmol, 1.0 equiv.) in benzene (3 ml/mmol) was added triethylamine (2.44 mmol, 2.0 equiv.) and the resulting reaction mixture was refluxed for 25 h. The mixture was cooled to room temperature and the solvent was evaporated under reduced pressure. The residue was dissolved in ethyl acetate and the organic layer was successively washed with water and brine. The organic layer was dried over sodium sulfate and the solvent was evaporated under reduced pressure to give the crude product which was purified by silica gel column chromatography. Yield: 51%.

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