Related Products of 112279-60-4,Some common heterocyclic compound, 112279-60-4, name is 4-Bromo-2,5-difluoroaniline, molecular formula is C6H4BrF2N, 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.
A mixture OF 4-(6-CHLORO-5-METHYL-PYRIMIDIN-4-YLOXY)-PIPERIDINE-1-CARBOXYLIC acid isopropyl ester (1.03 g, 3.28 mmol), palladium acetate (74 mg, 0.33 mmol), biphenyl-3-yl-di-tert-butyl- phosphane (9.7 mg, 0.033 mmol), sodium tert-butoxide (708 mg, 7.36 mmol), and 4-bromo-2,5- difluoro-phenylamine (706 mg, 3. 39 mmol) in 15 mL dioxane was heated in microwave for 1 hour at 120C. Solids were filtered off and mixture was purified by column chromatography (hexane/AcOEt) and crystallized from HEXANE/ACOET TO give compound A86 as a tanned solid (652 mg, 41%). 1H NMR (CDC13, 400 MHz) 5 1.04-1. 05 (d, 6H), 1.50-1. 61 (M, 2H), 1.74-1. 82 (M, 2H), 1.89 (s, 3H), 3.16-3. 22 (M, 2H), 3.51-3. 60 (M, 2H), 4.69-4. 76 (M, 1H), 5.09-5. 15 (M, 1H), 6.34-6. 36 (M, 1H), 7.07- 7.11 (M, 1H), 8.15 (s, 1H), 8. 34-8. 38 (M, 1H). Exact mass calculated for C2OH23BRF2N403 484.09, found 485.2 (MH).
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 4-Bromo-2,5-difluoroaniline, its application will become more common.
Reference:
Patent; ARENA PHARMACEUTICALS, INC.; WO2005/7647; (2005); A1;,
Bromide – Wikipedia,
bromide – Wiktionary