Electric Literature of 178876-83-0 ,Some common heterocyclic compound, 178876-83-0, molecular formula is C7H7BrN2O2, 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 degassed solution of methyl 6-amino-5-bromopyridine-2-carboxylate (1.06 g), ethyl acrylate (2.49 ml), tri-o-tolylphosphine (280 mg), triethylamine (3.18 ml) in dimethylformamide (50 ml) was added tris (dibenzylideneacetone) palladium (0) (211 mg) and the resultant solution was heated at 50C for 72h. After stirring overnight, the mixture was evaporated and the residue treated with dichloromethane (50 ml) and washed with H20. The aqueous fraction was re-extracted with 10% methanol in dichloromethane and the combined organic fractions dried (MgS04) and evaporated. Chromatography of the residue (60-80 petroleum ether-ethyl acetate 4: 1) gave the product (360 mg, 31 %). MS (+ve ion electrospray) m/z 251 (MH+, 100%)
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,178876-83-0, its application will become more common.
Reference:
Patent; SMITHKLINE BEECHAM P.L.C.; WO2003/87098; (2003); A1;,
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