Application of 128140-82-9,Some common heterocyclic compound, 128140-82-9, name is 1-(Difluoromethoxy)-4-iodobenzene, molecular formula is C7H5F2IO, 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 degassed mixture of 5-methyl-4-[4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-phenoxymethyl]-furan-2-carboxylic acid methyl ester (119) (200mg, 0.54mmoles), 4-difluoromethoxy-1-iodo-benzene (175mg, 0.65mmoles), 2M aqueous cesium carbonate (0.81ml) and), [1,1′-bis(diphenylphosphino)ferrocene]dichloropalladium(II) complex with dichloromethane (1 : 1) (20mg) in 1,4-dioxan (10ml), under an argon atmosphere was heated at 80C for 20h. Further quantities of 4-difluoromethoxy-1-iodo-benzene (87.5mg, 0.0.27mmoles) and [1,1′-bis(diphenylphosphino)ferrocene]dichloropalladium(II) complex with dichloromethane (1 : 1) (10mg) were added and heating at 80C was continued for 4 hours. After cooling, the mixture was concentrated. The residue was dissolved in dichloromethane and washed with water and brine, and dried. The solvent was evaporated and the residue was purified by flash chromatography using petrol (40-60)/diethyl ether 9 : 1v/v as eluent to afford compound 128 (120mg) as a wax. LC/MS System A ; Rt = 4.14 mins.
The synthetic route of 128140-82-9 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; PHARMAGENE LABORATORIES LIMITED; WO2004/67524; (2004); A1;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com