Реакция #10677

Уравнение реакции

Intermediate 132

4-[1-(4-methoxybenzyl)amino-5-isoquinolyl]amino-1-(tert-butoxycarbonyl)piperidine

→

title compound

Выход 99.6%

4-(1-amino-5-isoquinolyl)amino-1-(tert-butoxycarbonyl)piperidine

Выход 99.6%

Растворители

trifluoroacetic acid

Условия реакции

Обработка

1. 1
   Другоеthe solvent was evaporated under reduced pressure
2. 2
   workup.ADDITIONThe residue was added with dioxane (3 ml), 2 N aqueous sodium hydroxide (1 ml) and 2 di-t-butyl dicarbonate (393 mg)
3. 3
   ДругоеThe solvent was evaporated under reduced pressure
4. 4
   Другоеthe residue was purified by silica gel column chromatography (n-hexane:ethyl acetate:isopropylamine=5:5:1)

Методика

A solution of Intermediate 132 (270 mg) in 95% trifluoroacetic acid (5 ml) was stirred at 50° C. for 16 hours, and the solvent was evaporated under reduced pressure. The residue was added with dioxane (3 ml), 2 N aqueous sodium hydroxide (1 ml) and 2 di-t-butyl dicarbonate (393 mg) and stirred at room temperature for 1 hour. The solvent was evaporated under reduced pressure, and then the residue was purified by silica gel column chromatography (n-hexane:ethyl acetate:isopropylamine=5:5:1) to obtain the title compound (199 mg).

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