Reaktion #156484

ord-db28c7ff3749484faeef4530a43360f5

Lösungsmittel

Reaktionsbedingungen

Temperatur
150°CELSIUS
Detaillierte Bedingungen
See reaction.notes.procedure_details.

Aufarbeitung

  1. 1
    Sonstige5 min
  2. 2
    Waschenwashed with 10% Na2CO3 solution and brine
  3. 3
    FiltrationThe precipitate from the aqueous layer was filtered off
  4. 4
    Sonstigedried

Vorschrift

3-(3-Bromo-imidazo[1,2-a]pyridin-6-ylmethyl)-6-(1-methyl-1H-pyrazol-4-yl)-imidazo[1,2-b]pyridazine (Example 296, 80 mg, 0.196 mmol) was dissolved in DME (0.653 mL) with 3-cyanophenylboronic acid (28.2 mg, 0.196 mmol), 2 M Na2CO3 solution (0.353 mL, 0.705 mmol) and tetrakis(triphenylphosphine)palladium (11.3 mg, 0.010 mmol). The RM was heated at 150° C. 5 min under microwave irradiations. It was taken up with EtOAc and washed with 10% Na2CO3 solution and brine. The precipitate from the aqueous layer was filtered off and dried to afford the title compound as a grey solid (tR 0.8 min (conditions 2), MH+=431).

Quelle

DOI: 10.6084/m9.figshare.5104873.v1Patent: US08822468B2uspto-grants-2014_09