Réaction #44716

Équation de réaction

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

Solvants

toluene ethanol

Conditions de réaction

Traitement

1. 1
   AutreThe mixture is evaporated to dryness
2. 2
   Autrea rotary evaporator
3. 3
   Autrepurified by preparative HPLC

Mode opératoire

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.

Source