Electric Literature of 69038-76-2,Some common heterocyclic compound, 69038-76-2, name is 4-Bromo-N1-methylbenzene-1,2-diamine, molecular formula is C7H9BrN2, 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 solution of 4-bromo-N?-methylbenzene-1,2-diamine (1.7 g, 8 mmol) in triethyl orthoformate (10 mL) was added PTSA?H20 (152 mg, 0.8 mmol). The mixture was stirred at 85 C for 2 h, poured into H20 (50 mL) and extracted with EA (40 mL x 2). The organic layers were dried over anhydrous Na2SO4, filtered, concentrated in vacuo, and purified by silica gel column chromatography (PE/EA = 50/1 to 10/1) to afford 5-bromo-1-methyl-1H-benzo[djimidazole (1.5 g, 89 %) as a yellow solid. LC-MS mlz: 211.1 [M+Hf?. tR= 1.90 mm.
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 4-Bromo-N1-methylbenzene-1,2-diamine, its application will become more common.
Reference:
Patent; LYSOSOMAL THERAPEUTICS INC.; SKERLJ, Renato, T.; BOURQUE, Elyse Marie Josee; LANSBURY, Peter, T.; GOOD, Andrew, C.; (391 pag.)WO2017/176960; (2017); A1;,
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