Reaktion #49610

Reaktionsgleichung

4-chloro-5-(3-chloropropoxy)-7-[1-(tert-butoxycarbonyl)-5-(piperidin-1-ylmethyl)indol-2-yl]isoindolinone

4-hydroxypiperidine

water

→

4-chloro-5-[3-(4-hydroxypiperidin-1-yl)propoxy]-7-[1-(tert-butoxycarbonyl)-5-(piperidin-1-ylmethyl)indol-2-yl]isoindolinone

Ausbeute 80.1%

Lösungsmittel

N,N-dimethylacetoamide

Reaktionsbedingungen

Aufarbeitung

1. 1
   FiltrationThe obtained solid was collected by filtration
2. 2
   Waschenwashed with water
3. 3
   Sonstigeby drying under reduced pressure

Vorschrift

In a similar manner to Step 2 of Example 440, 4-chloro-5-(3-chloropropoxy)-7-[1-(tert-butoxycarbonyl)-5-(piperidin-1-ylmethyl)indol-2-yl]isoindolinone (90.2 mg, 0.158 mmol) was dissolved in N,N-dimethylacetoamide (0.9 mL), and the solution was treated with 4-hydroxypiperidine (159 mg, 1.58 mmol). The reaction mixture was added with water. The obtained solid was collected by filtration and washed with water, followed by drying under reduced pressure to obtain 4-chloro-5-[3-(4-hydroxypiperidin-1-yl)propoxy]-7-[1-(tert-butoxycarbonyl)-5-(piperidin-1-ylmethyl)indol-2-yl]isoindolinone (80.6 mg, yield 80%).

Quelle