These common heterocyclic compound, 239135-53-6, name is 2-Fluoro-4-iodo-1-(trifluoromethyl)benzene, 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. Recommanded Product: 239135-53-6
Intermediate 79: 3,4-bis(Benzyloxy)-6-[(E)-2-[3-fluoro-4-(trifluoromethyI)- phenyl]ethenyl]pyridazine A vessel containing 3,4-bis(benzyloxy)-6-ethenylpyridazine (Intermediate 78, 1.09 g, 3.42 mmol), tris-(2-methylphenyl)phosphane (0.208 g, 0.685 mmol), 2-f.uoro-4-iodo-l- (trifluoromethyl)benzene (1.191 g, 4.1 1 mmol) and palladium(II) acetate (0.038 g, 0.171 mmol) was evacuated and acetonitrile (10 ml) and triethylamine (9.07 ml, 65.1 mmol) were added in vacuo and then the mixture was flushed with nitrogen. The reaction was then heated in the microwave at 80 C for 4 hours and, upon cooling, was diluted with dichloromethane and washed with saturated aqueous ammonium chloride solution. The organics were dried ( gSC^), filtered and solvent removed in vacuo to give a brown oil which was purified by column chromatography (silica, eluting with 30- 100 % dichloromethane in petrol) to yield 3,4-bis(benzyloxy)-6-[(E)-2-[3-fiuoro-4- (trifluoromethyl)phenyl]ethenyl]pyridazine (1.1 g, 2.29 mmol, 67 % yield). 1H NMR (CDCI3) delta 7.53 – 7.68 (m, 3 H), 7.31 – 7.53 (m, 12 H), 6.97 (s, 1 H), 5.71 (s, 2 H) and 5.28 (s, 2 H). MS ES+: 481.
The synthetic route of 2-Fluoro-4-iodo-1-(trifluoromethyl)benzene has been constantly updated, and we look forward to future research findings.
Reference:
Patent; TAKEDA PHARMACEUTICAL COMPANY LIMITED; FARNABY, William; FIELDHOUSE, Charlotte; HAZEL, Katherine; KERR, Catrina; KINSELLA, Natasha; LIVERMORE, David; MERCHANT, Kevin; MILLER, David; WO2013/27000; (2013); A1;,
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