Synthetic Route of 937046-98-5,Some common heterocyclic compound, 937046-98-5, name is 7-Bromopyrrolo[2,1-f][1,2,4]triazin-4-amine, molecular formula is C6H5BrN4, 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.
Into a 250-mL round-bottom flask purged and maintained with an inert atmosphere of argon, was placed a solution of compound 2a (3.2 g, 15.02 mmol) in THF (40 mL). n-Butyllithium (18.75 mL, 1.6 N in THF) was added dropwise at -78C, and then chloro[2-(chlorodimethylsilyl)ethyl]dimethylsilane (3.2 g, 14.87 mmol) was added at -78 C. After the resulting solution was stirred for 0.5 hours at -78 C, n- butyllithium (6.25 mL, 1.6 N in THF) was added. After the resulting mixture was stirred for 5 minutes, a solution of compound lh (3.7 g, 9.75 mmol) in THF (10 mL) was added to the mixture and the resulting solution was stirred for 2 hours at -78C. After that the reaction was quenched by the addition of 30 mL saturated aqueous solution of ammonium chloride, extracted with ethyl acetate (3×150 mL), dried over anhydrous sodium sulfate and concentrated in vacuo. The residue was applied onto a silica gel column and eluted with ethyl acetate/petroleum ether (1 :20~1 :3) to provide 350 mg (7%) of compound 2c as an off-white solid. LC-MS: (ES, m/z): 514.0 [M+H]+
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 7-Bromopyrrolo[2,1-f][1,2,4]triazin-4-amine, its application will become more common.
Reference:
Patent; MERCK SHARP & DOHME CORP.; GIRIJAVALLABHAN, Vinay; BOGEN, Stephane; PAN, Weidong; DANG, Qun; DAVIES, Ian; WO2014/59901; (2014); A1;,
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