تفاعل #44715

ord-f49be5af1312475ea5319a61adc24c3e

معادلة التفاعل

O=C([O-])O.[Na+]
sodium bicarbonate
Nc1ccc(Oc2ccc3[nH]ncc3c2)c(F)c1
5-(4-amino-2-fluorophenoxy)-1H-indazole
Nc1ccc(Oc2ccc3[nH]ncc3c2)c(F)c1
5-(4-Amino-2-fluorophenoxy)-1H-indazole
Nc1nc(Cl)cc(Cl)n1
4,6-dichloro-2-pyrimidineamine
Cl
hydrogen chloride
Nc1nc(Cl)cc(Nc2ccc(Oc3ccc4[nH]ncc4c3)c(F)c2)n1
N-[2-Amino-6-chloro-4-pyrimidinyl]-N-[3-fluoro-4-(1H-indazol-5-yloxy)phenyl]amine

المذيبات

ظروف التفاعل

درجة الحرارة
100°CELSIUS
الظروف التفصيلية
See reaction.notes.procedure_details.

المعالجة

  1. 1
    استخلاصextracted 3× with ethyl acetate
  2. 2
    تجفيفThe organic phase is dried with sodium sulfate
  3. 3
    تركيزconcentrated
  4. 4
    أخرىa rotary evaporator

الإجراء التجريبي

1.65 g (6.78 mmol) of 5-(4-amino-2-fluorophenoxy)-1H-indazole (from example XII) are suspended in 90 ml of water. 1.11 g (6.78 mmol) of 4,6-dichloro-2-pyrimidineamine and 0.68 ml of concentrated aqueous hydrogen chloride solution are added, and the mixture is stirred at 100° C. overnight. For work-up, the reaction solution is made alkaline with saturated sodium bicarbonate solution and extracted 3× with ethyl acetate. The organic phase is dried with sodium sulfate and concentrated using a rotary evaporator.

المصدر

DOI: 10.6084/m9.figshare.5104873.v1براءة الاختراع: US07737153B2uspto-grants-2010_06