Synthetic Route of 78581-99-4, In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. 78581-99-4, name is 5,6-Difluorobenzimidazole belongs to imidazoles-derivatives compound, it is a common compound, a new synthetic route is introduced below.
To a solution of (lR,3S,5S,6r)-6-(((S)-l,l-dimethylethylsulfinamido)methyl) bicyclo[3.1.0]hexan-3-yl methanesulfonate (1.42 g, 4.59 mmol) in THF (15.30 mL) was added cesium carbonate (4.49 g, 13.77 mmol) and 5,6-difluoro-lH-benzo[d]imidazole (0.849 g, 5.51 mmol) and the resulting mixture was stirred at 85C for 16 h. The reaction was cooled to RT, concentrated, diluted with water and extracted twice with EtOAc. The organics were washed with brine, combined, dried over MgS04, concentrated and purified by flash chromatography (5 to 40% of 80:20:2 EA:EtOH:NH40H in hexanes) to give (S)-N- (((lR,3R,5S,6r)-3-(5,6-difluoro-lH-benzo[d]imidazol-l-yl)bicyclo[3.1.0]hexan-6-yl)methyl)- 2-methylpropane-2-sulfinamide (1.03 g, 2.80 mmol, 61.1 % yield) as a white solid. MS (ES+) C18H23F2N3OS requires: 367, found: 368 [M+H]+.
The synthetic route of 5,6-Difluorobenzimidazole has been constantly updated, and we look forward to future research findings.
Reference:
Patent; TESARO, INC.; LEWIS, Richard, T.; HAMILTON, Matthew; JONES, Philip; PETROCCHI, Alessia; REYNA, Naphtali; CROSS, Jason; HAN, Michele; SOTH, Michael; MCAFOOS, Timothy; TREMBLAY, Martin; (356 pag.)WO2018/136437; (2018); A2;,
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