Some common heterocyclic compound, 72373-82-1, name is 1-Chloro-2-fluoro-3-iodobenzene, molecular formula is C6H3ClFI, 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. category: iodides-buliding-blocks
To a solution of 5-{4-[(S)-1-(3-fluoropropyl)pyrrolidin-3-yloxy]phenyl}-6-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-8,9-dihydro-7H-benzocyclohepten-2-ol (D’) (100.3 mg, 197.66 mumol), in dioxane (1 ml) and water (0.5 ml), was added 3-chloro-2-fluoroiodobenzene (60.83 mg, 237.19 mumol), Cs2CO3 (128.93 mg, 395.31 mumol) and Pd(dppf)Cl2 (9.68 mg, 11.86 mumol). The reaction mixture was heated at 70° C. for 6 hours, and partitioned between DCM and water. The aqueous phase was washed with DCM and organic phases were dried and concentrated under reduced pressure. The residue was purified by column chromatography eluting with a gradient of MeOH in DCM (0percent to 10percent) to give a solid which was further purified on strong cation exchange (SCX) column to give 18 mg (18percent) of 6-(3-chloro-2-fluorophenyl)-5-[4-[(3S)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7H-benzo[7]annulen-2-ol.
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 72373-82-1, its application will become more common.