These common heterocyclic compound, 2613-34-5, name is 3-Chloro-2,4-difluoroaniline, 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. 2613-34-5
3-CHLORO-2, 4-DIFLUOROANILINE (1.7 g, 10.1 mmol) and 5N hydrogen chloride in isopropanol (2 ml) were added to a suspension of tert-butyl 4- [ (4-CHLORO-7-METHOXYQUINAZOLIN-6- yl) oxy] PIPERIDINE-1-CARBOXYLATE (4 g, 10.1 mmol, PCT Int. Appl. W02003082831, AstraZeneca) in isopropanol (50 ml). The mixture was stirred at 80C for 3 hours. After evaporation of the solvents, the residue was purified by chromatography on silica gel (eluant: 5-10% 7N methanolic ammonia in dichloromethane) to give 4- (3-CHLORO-2, 4-difluoroanilino) – 7-METHOXY-6-[(PIPERIDIN-4-YL) OXY] QUINAZOLINE (3.63 g, 85%) as a white solid. HNMR Spectrum: (CDC13 + CD3CO2D) : 2.15 (m, 2H), 2.30 (m, 2H), 3.34 (m, 2H), 3.47 (m, 2H), 4.01 (s, 3H), 4.91 (m, 1H), 7.03 (m, 1H), 7.58 (m, 2H), 7.90 (s, 1H), 8.55 (s, 1H) ; Mass spectrum: MH+ 421.
Chemical properties determine the actual use. Each compound has specific chemical properties and uses. We look forward to more synthetic routes in the future to expand reaction routes of 2613-34-5.
Reference:
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2005/28470; (2005); A1;,
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