A new synthetic route of 5-Cyanopicolinic acid

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,53234-55-2, its application will become more common.

Reference of 53234-55-2 ,Some common heterocyclic compound, 53234-55-2, molecular formula is C7H4N2O2, 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.

Step 15To a solution of compound 9-15 (63 mg, 0.21 mmol) in CH2C12 (2 ml) were added 5-cyanopicolinic acid hydrate (38.2 mg, 0.23 mmol), EDC (48 mg, 0.25 mmol) and 2 mmol L HC1 (aqueous solution, 0.11 ml, 0.209 mmol) at room temperature. After stirring for 1 h at the same temperature, the reaction mixture was treated with H20. The aqueous layer was extracted with AcOEt, and the organic layer was dried over MgS04, filtered and concentrated. The crude product was added to a silica gel column and eluted with hexane/EtOAc 30% to 70%. Collected fractions were evaporated to afford compound 1-35 (66 mg, 0.153 mmol, 73%) as a white solid.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,53234-55-2, its application will become more common.

Reference:
Patent; SHIONOGI & CO., LTD.; KUSAKABE, Ken-ichi; TADANO, Genta; KOMANO, Kazuo; FUCHINO, Kouki; NAKAHARA, Kenji; WO2015/156421; (2015); A1;,
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