Related Products of 1003-99-2, These common heterocyclic compound, 1003-99-2, name is 2-Bromo-5-fluoroaniline, 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.
The N-(t-butyloxycarbonyl)-4-piperidone (10.13 g, 50.8 mmol, 1.0 eq) and the 2-bromo-5-fluoroaniline (11.6Og, 61.0 mmol, 1.2 eq.) were weighed into a flask. Acetic acid (75 mL) was added, followed by trimethylsilyl cyanide (7.75 mL, 58.1 mmol, 1.14 eq.). The mixture was stirred at rt for 24 hr, and was then added to a mixture of 200 mL ice and 200 mL saturated ammonium hydroxide solution. The resulting mixture was extracted twice with methylene chloride, and the organic solution was dried over magnesium sulfate, filtered, and concentrated to provide 22.57g of crude product.
Statistics shows that 2-Bromo-5-fluoroaniline is playing an increasingly important role. we look forward to future research findings about 1003-99-2.
Reference:
Patent; MERCK & CO., INC.; SUNESIS PHARMACEUTICALS, INC.; WO2006/44497; (2006); A2;,
Bromide – Wikipedia,
bromide – Wiktionary