Synthetic Route of 1097871-23-2, These common heterocyclic compound, 1097871-23-2, name is 1-Chloro-2,5-difluoro-4-iodobenzene, 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.
Copper(I) iodide (69.4 mg, 0.364 mmol), 2-phenylphenol (93.0 mg, 0.546 mmol) and cesium carbonate (1.78 g, 5.46 mmol) were added to a dry flask under nitrogen. Ethyl malonate (1.11 mL, 7.29 mmol) was added to the mixture, followed by l-chloro-2,5-difluoro-4- iodobenzene (1.00 g, 3.64 mmol) in tetrahydrofuran (3.64 mL, 44.9 mmol). The reaction mixture was sealed and heated to 90C. After 12 hours, the reaction mixture was allowed to cool to room temperature and then diluted with saturated NH4Cl and EtOAc. The organic layer was separated, dried and filtered through Celite. The brown oil was purified via silica gel chromatography (0-30% EtOAc-hexane) to give diethyl 2-(4-chloro-2,5-difluorophenyl)malonate (0.65 g, 58%). 1H NMR (400 MHz, CDCl3) delta 7.37 (dd, J = 6.3, 9.3, IH), 7.17 (dd, J = 6.1, 8.9, IH), 4.91 (s, IH), 4.33 – 4.14 (m, 4H), 1.28 (t, J = 7.2, 6H).
The synthetic route of 1097871-23-2 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; ARRAY BIOPHARMA INC.; GENENTECH, INC.; WO2009/6567; (2009); A2;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com