Electric Literature of 89830-98-8, These common heterocyclic compound, 89830-98-8, name is 5-Cyclopropyl-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.
To a suspension of 7-iodo-6-methyl-3,4-dihydro-2H-isoquinolin-1-one (446.0 mg, 1.476 mmol), 4-cyclopropyl-1H-imidazole (218.4 mg, 1.919 mmol) in DMSO (2.5 mL) is added K2C03 (0.408 g, 2.952 mmol). The mixture is degassed with a stream of N2 for 5minutes. L-Proline (0.034 g, 0.295 mmol) and CuT (0.0562 g, 0.295 mmol) are added sequentially and the resulting mixture is stirred at 130 C for 5 hours under microwave conditions. The reaction mixture is slowly quenched with water (30 mL). The aqueous phase is extracted with EtOAc (2×80 mL) and washed with saturated brine (25 mL). The organic extracts are dried over Na2 SO4, filtered, and evaporated to dryness. The crude product is purified by silica gel flash chromatography, eluting with a gradient of 0% to 4% MeOH in DCM to give the title compound (0.198 g, 47.68%) as a white solid. ES/MS (m/z):268.0 (M+H).
Statistics shows that 5-Cyclopropyl-1H-imidazole is playing an increasingly important role. we look forward to future research findings about 89830-98-8.
Reference:
Patent; ELI LILLY AND COMPANY; LILLY CHINA RESEARCH AND DEVELOPMENT CO., LTD; LEI, Hui; LIU, Gang; TIAN, Yuan; ZHANG, Haizhen; (0 pag.)WO2018/160406; (2018); A1;,
Imidazole – Wikipedia,
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