Reacción #79074

Ecuación de reacción

NaHCO3

7-amino-4-methylthiopyrido[4,3-d]pyrimidine

2-aminobenzotrifluoride hydrochloride

2-aminobenzotrifluoride

→

7-amino-4-(2-trifluoromethylanilino)pyrido[4,3-d]pyrimidine

Rendimiento 41.0%

Disolventes

MeOH CHCl3

Condiciones de reacción

Tratamiento posterior

1. 1
   Otrodried onto silica gel
2. 2
   Otrochromatographed over silica gel (6-7%; MeOH/CH2Cl2)

Procedimiento

A mixture of 7-amino-4-methylthiopyrido[4,3-d]pyrimidine (300 mg, l.56 mmol), 2-aminobenzotrifluoride hydrochloride (1.00 g, 5.06 mmol) and 2-aminobenzotrifluoride (2.00 g, 12.4 mmol) is stirred at 160° C. for 10 min. The resulting product is neutralized with excess NaHCO3, dissolved in MeOH/CHCl3, dried onto silica gel and chromatographed over silica gel (6-7%; MeOH/CH2Cl2) to give 7-amino-4-(2-trifluoromethylanilino)pyrido[4,3-d]pyrimidine (194 mg, 41%) as a cream solid, mp (MeOH/CHCl3/light petroleum) 126-130 ° C. (dec.). 1H NMR (DMSO) δ 10.60 (1H, brs), 9.17 (1H, brs), 8.13 (1H, brs), 7.76, 7.69 (1H, 1H, m, m), 7.45 (2H, m), 6.66 (2H, brs), 6.36 (1H, s).

Fuente