Application of 2265-91-0,Some common heterocyclic compound, 2265-91-0, name is 1,3-Difluoro-5-iodobenzene, molecular formula is C6H3F2I, 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.
Intermediate 4: Ethyl 1-(3,5-difluorophenyl)-5-methyl-1/-/-1 ,2,3-triazole-4-carboxylate; To a mixture of 1 ,3-difluoro-5-iodobenzene (0.2 g, 0.833 mmol) and ethyl 2- butynoate (0.097 ml, 0.833 mmol) in water/DMSO (0.22ml/2ml) at room temperature was added L-proline (0.019 g, 0.167 mmol), sodium carbonate (0.018 g, 0.167 mmol), sodium azide (0.065 g, 1.000 mmol), sodium l-ascorbate (0.017 g, 0.083 mmol) and copper(ll) sulfate pentahydrate (10.40 mg, 0.042 mmol) (in this order) and the mixture was heated at 65C overnight. Monitoring by LC/MS revealed starting material to be present and so the temperature was increased to 100 degrees and the mixture was heated overnight at lOOdegC. On cooling to room temperature, the mixture was quenched with aqueous ammonia (1 ml) and EtOAc (20ml) and water
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 1,3-Difluoro-5-iodobenzene, its application will become more common.