Synthetic Route of 207346-42-7, These common heterocyclic compound, 207346-42-7, name is Methyl 2-amino-4,5-difluorobenzoate, 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.
Example 2; Synthesis of f4-(6-fluoro-7-methylamino-2,4-dioxo-l,4-dihydro-2H- quinazolin-3-yI)-phenyll-5-chloro-thiophen-2-yl-sulfonyIurea (7a)Step i.Ia 2a 2b[0276] Aniline 1 (1H NMR (DMSO): delta 7.58 (dd, IH), 6.72 (dd, IH), 3.77 (s, 3H); 6.0 g, 32.085 mmol) was placed in a 500 mL round bottomed flask and 20% phosgene in toluene (175 mL, 332.50 mmol, 10.36 equiv) was added. The resulting somewhat sticky suspension was then magnetically stirred overnight at room temperature resulting in a clear, colorless solution. An aliquot removed, blown dry with argon, quenched with MeOH, and analyzed by RP-HPLC/MS to show no unreacted aniline 1 and clean formation of the isocyanate 2a and/or carbamoyl chloride 2b as analyzed as its methyl-carbamate. The mixture was concentrated first by rotary evaporation and then under high vacuum to yield 6.76g (99% yield) of the isocyanate 2a and/or carbamoyl chloride 2b as a free-flowing white solid.
Statistics shows that Methyl 2-amino-4,5-difluorobenzoate is playing an increasingly important role. we look forward to future research findings about 207346-42-7.
Reference:
Patent; PORTOLA PHARMACEUTICALS, INC.; WO2008/137809; (2008); A2;,
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