Electric Literature of 640280-28-0,Some common heterocyclic compound, 640280-28-0, name is 1-Bromo-2-iodo-4-(trifluoromethyl)benzene, molecular formula is C7H3BrF3I, 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.
Cs2CO3 (926 mg, 2.84 [MMOL),] Pd2 (dba) 3 (104 mg, 0.114 mmol), [2-DICYCLOHEXYLPHOSPHINO-2′-] (N, N-dimethylamino) biphenyl (36 mg, 0.091 mmol), anhydrous toluene (5 mL), methyl 2- amino-5-cyanobenzoate [PHA-522499] (200 mg, 1.136 mmol), 1-iodo-2-bromo-5- trifluoromethylbenzene [PHA-738728] (400 mg, 1.136 [MMOL).] The mixture is heated at [65 C] for 66 h. The resulting mixture is cooled to room temperature and filtered through [CELITE (E).] The filtrate is concentrated and purified by flash chromatography. The yield is 65mg of methyl 5-cyano-2-{[2-{[4-cyano-2-(methoxycarbonyl) phenyl] amino}-4- (trifluoromethyl) phenyl] amino} benzoate, 13%. MS (ESI-) for [C25HI7F3N404] [NT/Z] 493 (M-H)-. ‘H NMR (400 MHz, CDCl3) 8 9.93 (bs, [1] H), 9.83 (bs, [1] H), 8.22 [(M,] 2 H), 7.69 (bs, [1] H), 7.52 [(M,] 4 H), 7.05 (m, [1] H), 6.81 (m, [1] H), 3.84 (s, 3 H), 3.86 (s, 3 H).
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 1-Bromo-2-iodo-4-(trifluoromethyl)benzene, its application will become more common.
Reference:
Patent; PHARMACIA & UPJOHN COMPANY; PHARMACIA ITALIA S.P.A; WO2004/2940; (2004); A1;,
Iodide – Wikipedia,
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