Reaktion #49604

ord-515395442a7e4b0a9bb8e74c3465488f

Reaktionsbedingungen

Temperatur
90°CELSIUS
Detaillierte Bedingungen
See reaction.notes.procedure_details.

Aufarbeitung

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

Vorschrift

4-Chloro-5-(3-chloropropoxy)-7-[1-(tert-butoxycarbonyl)-5-(piperidin-1-ylmethyl)indol-2-yl]isoindolinone (90.4 mg, 0.158 mmol) was dissolved in N,N-dimethylacetoamide (1.0 mL), and the solution was added with 2-(ethylamino)ethanol (0.321 mL, 2.37 mmol), followed by stirring at 90° C. for 72 hours. 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-[N-ethyl(2-hydroxyethyl)amino]propoxy]-7-[1-(tert-butoxycarbonyl)-5-(piperidin-1-ylmethyl)indol-2-yl]isoindolinone (79.8 mg, yield 81%).

Quelle

DOI: 10.6084/m9.figshare.5104873.v1Patent: US07745641B2uspto-grants-2010_06