Reference of 71759-87-0, These common heterocyclic compound, 71759-87-0, name is 4-Iodo-1-methyl-1H-imidazole, 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.
Procedure E3c – {3-r7-(1-Methyl-1 H-imidazol-4-yl)-imidazori ,2-alpyridin-3-yll-phenyl}-3-(2.2,2-trifluoro-ethyl)-urea; Procedure E3c is using the conditions described in generic Suzuki A4eTo a stirred mixture of 1-[3-(7-Boronic acid -imidazo[1 ,2-a]pyridn-3-yl)-phenyl]-3-(2,2,2- trifluoro-ethyl)-urea (0.15g, 0.39 mmol), in a MW tube was added 4-iodo-1-methyl-1 H- imidazole (83mg, 0.39mmol), SPHOS (6.5mg, 0.016mmol) and Pd2(dba)3 (7mg, 0.0076mmol ) in dioxane (2ml) followed by K3PO 4 (252mg, 1.18mmol) in water (1.2ml). The reaction mixture was heated in a CEM discover microwave synthesizer (300W) at 120 0C for hr. The mixture was allowed to cool, then partitioned between EtOAc /H2O, the organic layer was separated, dried (MgSO4), filtered and the solvent removed in vacuo. The residue was purified by prep HPLC to afford the desired product (8mg) MS: [M+H]+ = 415.To a stirred mixture of 1-[3-(7-Boronic acid -imidazo[1 ,2-a]pyridn-3-yl)-phenyl]-3-(2,2,2- trifluoro-ethyl)-urea (0.15g, 0.39 mmol), in a MW tube was added 4-iodo-1-methyl-1 H- imidazole (83mg, 0.39mmol), SPHOS (6.5mg, 0.016mmol) and Pd2(dba)3 (7mg, 0.0076mmol ) in dioxane (2ml) followed by K3PO 4 (252mg, 1.18mmol) in water (1.2ml). The reaction mixture was heated in a CEM discover microwave synthesizer (300W) at 120 0C for hr. The mixture was allowed to cool, then partitioned between EtOAc /H2O, the organic layer was separated, dried (MgSO4), filtered and the solvent removed in vacuo. The residue was purified by prep HPLC to afford the desired product (8mg) MS: [M+H]+ = 415.
Statistics shows that 4-Iodo-1-methyl-1H-imidazole is playing an increasingly important role. we look forward to future research findings about 71759-87-0.
Reference:
Patent; ASTEX THERAPEUTICS LIMITED; WO2008/78091; (2008); A1;,
Imidazole – Wikipedia,
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