Reaktion #44716

Reaktionsgleichung

N-[2-amino-6-chloro-4-pyrimidinyl]-N-[3-fluoro-4-(1H-indazol-5-yloxy)phenyl]amine

N-[2-Amino-6-chloro-4-pyrimidinyl]-N-[3-fluoro-4-(1H-indazol-5-yloxy)phenyl]amine

phenylboronic acid

sodium carbonate

→

N-(2-Amino-6-phenyl-4-pyrimidinyl)-N-[3-fluoro-4-(1H-indazol-5-yloxy)phenyl]amine

Lösungsmittel

toluene ethanol

Reaktionsbedingungen

Aufarbeitung

1. 1
   SonstigeThe mixture is evaporated to dryness
2. 2
   Sonstigea rotary evaporator
3. 3
   Sonstigepurified by preparative HPLC

Vorschrift

50 mg (130 μmol) of N-[2-amino-6-chloro-4-pyrimidinyl]-N-[3-fluoro-4-(1H-indazol-5-yloxy)phenyl]amine (from example 8) are suspended in 3 ml of toluene/ethanol (2:1), and 4.68 mg of tetrakis(triphenylphosphine)palladium(0) are added. After addition of 19.7 mg (160 μmol) of phenylboronic acid and 0.50 ml of 2M aqueous sodium carbonate solution, the mixture is stirred at 100° C. overnight. The mixture is evaporated to dryness using a rotary evaporator and purified by preparative HPLC.

Quelle