Some common heterocyclic compound, 103962-05-6, name is 1-Iodo-4-(trifluoromethoxy)benzene, molecular formula is C7H4F3IO, 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. Safety of 1-Iodo-4-(trifluoromethoxy)benzene
To a solution of compound 02-5-1 (1.00 g, 3.0 mmol, 1.0 eq) in DMA (5 mL) was added 1-iodo-4-(trifluoromethoxy)benzene (1.73 g, 6.0 mmol, 939 muL, 2.0 eq), PdCl2 (10.6 mg, 60.0 mumol, 0.02 eq), 1,10-phenanthroline (10.8 mg, 60.0 mumol, 0.02 eq), Ag2CO3 (1.24 g, 4.50 mmol, 204 muL, 1.5 eq) and K3PO4 (1.27 g, 6.0 mmol, 2.0 eq). The suspension was degassed under vacuum and purged with N2 several times. The mixture was stirred at 150 °C for 12 h. The reaction mixture was poured into H2O (100 mL), filtered through Celite, and washed with EtOAc (50 mL). The filtrate was extracted with EtOAc (100 mL*3). The combined organic layers were washed with brine (100 mL*2), dried over anhydrous Na2SO4, filtered and concentrated under reduced pressure. The residue was purified by column chromatography (SiO2) to give compound 02-5-2 (300.0 mg, 608 mumol, 20percent yield).
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 103962-05-6, its application will become more common.
Reference:
Patent; KYRAS THERAPEUTICS, INC.; VACCA, Joseph P.; LI, Dansu; (587 pag.)WO2017/96045; (2017); A1;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com