452-68-6, These common heterocyclic compound, 452-68-6, name is 1-Fluoro-4-iodo-2-methylbenzene, 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.
EXAMPLE 9 Ethyl Z-(1R’,3S’)-3-(4-fluoro-3-methylphenyl)-2-[3-(5-methyl-2-m-tolyloxazol-4-yl-methoxy)cyclohexyloxymethyl]acrylate 220 mg of tetrabutylammonium chloride and 332 mg of potassium carbonate are suspended in 4 ml of dimethylformamide and stirred intensively for 20 min. 400 mg of ethyl (1R,3S)-2-[3-(5-methyl-2-m-tolyloxazol-4-ylmethoxy)cyclohexyloxy-methyl ]acrylate, 25 mg of triphenylphosphine and 212 mg of 4-fluoro-3-methyliodo-benzene are added, the mixture is degassed and vented with argon and 10 mg of palladium acetate and 0.2 mol of water are added. The mixture is heated at 60 C for 4 h. After cooling, 20 ml of ethyl acetate and 50 ml of sat. NaCI solution are added. The organic phase is dried over sodium sulfate, the solvent is removed under reduced pressure and the residue is purified by flash chromatography on silica gel (n-heptane/ethyl acetate=4:1). This gives ethyl Z-(1R’,3S’)-3-(4-fluoro-3-methylphenyl)-2-[3-(5-methyl-2-m-tolyloxazol-4-ylmethoxy)cyclohexyloxymethyl ]-acrylate as a colorless oil. C31H38FNO5 (523.65), MS (ESI): 524 (M+H+).
Chemical properties determine the actual use. Each compound has specific chemical properties and uses. We look forward to more synthetic routes in the future to expand reaction routes of 452-68-6.
Reference:
Patent; Aventis Pharma Deutschland GmbH; US2004/209920; (2004); A1;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com