Reference of 1978-39-8, These common heterocyclic compound, 1978-39-8, name is 5-Fluoro-2-methoxyaniline, 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.
8-Fluoro-5-methoxy-2H-benzoreiri ,2,41thiadiazin-3(4H)-one 1 ,1 -dioxide (lnt-12) (2152) A 250 mL round-bottomed flask was charged with chlorosulfonyl isocyanate (2.058 ml) in nitropropane (20 ml) to give a colorless solution at -40 C under nitrogen. After 10 min, a solution of 5-fluoro-2-methoxyaniline (2.72 g) in nitropropane (10 ml) was added to the reaction mixture. After 10 min, the reaction was warmed to 0 C. After 1 h, aluminum chloride (3.21 g) was added to the reaction mixture. After 5 min, the reaction mixture was warmed to 1 10 C. After 30 min, the reaction mixture was poured in ice/water (400 mL) and stirred for 1 h. The solids were filtered and washed with water. The solids were placed in drying oven overnight at 50 C to obtain the titled compound (2.3 g). LCMS m/z 247.1 (M+H).
The synthetic route of 1978-39-8 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED; ADAMS, Jerry Leroy; ATOR, Laura E.; DUFFY, Kevin J.; GRAYBILL, Todd L.; KIESOW, Terence John; LIAN, Yiqian; MOORE, Michael Lee; RALPH, Jeffrey M.; RIDGERS, Lance Howard; (370 pag.)WO2017/98421; (2017); A1;,
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