Реакция #72094

Уравнение реакции

Methyl cis(±)-5-(4-{[(benzyloxy)carbonyl]amino}-3-methoxypiperidin-1-yl)-2-methylthiophene-3-carboxylate

hydrobromic acid acetic acid

→

title compound

Выход 59.0%

Methyl cis(±)-5-(4-amino-3-methoxypiperidin-1-yl)-2-methylthiophene-3-carboxylate

Выход 59.0%

Растворители

ethyl acetate

acetic acid

Условия реакции

Обработка

1. 1
   Промывкаwashed with water and brine
2. 2
   Сушкаdried over anhydrous sodium sulfate
3. 3
   Концентрированиеconcentration under reduced pressure
4. 4
   Другоеthe residue was purified by silica gel column chromatography (elution solvent: methanol/ethyl acetate=0, 10%)

Методика

Methyl cis(±)-5-(4-{[(benzyloxy)carbonyl]amino}-3-methoxypiperidin-1-yl)-2-methylthiophene-3-carboxylate obtained in Example (188c) (50 mg) was dissolved in acetic acid (1 mL). A hydrobromic acid-acetic acid solution (1 ml) was added, and the mixture was stirred at room temperature for one hour. The reaction solution was diluted with ethyl acetate, washed with water and brine, and dried over anhydrous sodium sulfate. Following concentration under reduced pressure, the residue was purified by silica gel column chromatography (elution solvent: methanol/ethyl acetate=0, 10%) to obtain 20 mg of the title compound as a glassy solid (59%).

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