Electric Literature of 63558-65-6 ,Some common heterocyclic compound, 63558-65-6, molecular formula is C4H2ClIN2, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc., below Introduce a new synthetic route.
To a solution of 4-amino-2,5-difluorophenol (0.190 g, 1.310 mmol) in DMF ( 10 mL) was added potassium ter/-butoxide (0.168 g, 1.497 mmol). The mixture was stirred at RT for 30 min. 4-Chloro-5-iodopyrimidine (0.30 g, 1.248 mmol) was added and the reaction mixture was heated at 80 C overnight. The reaction mixture was quenched with water and the solution was extracted with EtOAc (3x). The organic solution was washed with 5% aqueous lithium chloride solution and brine. The organics were dried over gS04, filtered, and concentrated. The crude was purified by silica gel column chromatography ( 10% to 50%EtOAc/hexane) to obtain 2,5-difluoro-4-(5-iodopyrimidin-4-yloxy)benzenamine (160 mg, 36.7%) yield) which was used for the next reaction. MS (ESI) m/z: 349.9 (M+H+).
In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles. 63558-65-6, 4-Chloro-5-iodopyrimidine, other downstream synthetic routes, hurry up and to see.
Reference:
Patent; DECIPHERA PHARMACEUTICALS, LLC; FLYNN, Daniel, L.; KAUFMAN, Michael, D.; WO2011/139891; (2011); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia