Electric Literature of 884494-45-5 ,Some common heterocyclic compound, 884494-45-5, molecular formula is C6H5FIN, 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 mixture of racemic 1-(1H-indazol-6-yl)spiro[2.2lpentane-1-carbonitrile (300 mg, 1.43 mmol) (Q.3), 2-fluoro-4-iodo-6-methylpyridine (510 mg, 2.15 mmol), trans-N ,N?-dimethyl- 1,2-cyclohexanediamine (61.2 mg, 0.430 mmol), copper(I) iodide (82 mg, 0.43 mmol), and cesium carbonate (934 mg, 2.87 mmol) in a 20 mL microwave vial, was added DMSO (2 mL). The vial was sealed, degassed and backfilled with nitrogen (3x) and stirred at 50C overnight. The mixture was diluted with water (5 mL), and extracted with DCM (3 x 5 mL). The organic extracts were combined, dried over MgSO4 and concentrated to dryness. The residue waspurified by silica gel column chromatography (gradient elution: 0-50% EtOAc)/hexanes).
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,884494-45-5, its application will become more common.
Reference:
Patent; MERCK SHARP & DOHME CORP.; CANDITO, David Annunziato; GRAHAM, Thomas, H.; ACTON, John; CHAU, Ryan Wing-Kun; CHEN, Joanna, L.; ELLIS, J. Michael; FULLER, Peter, H.; GULATI, Anmol; GUNAYDIN, Hakan; KATTAR, Solomon; KEYLOR, Mitchell Henry; LAPOINTE, Blair, T.; LIU, Ping; LIU, Weiguo; METHOT, Joey, L.; NEELAMKAVIL, Santhosh, F.; SIMOV, Vladimir; TONG, Ling; WOOD, Harold, B.; (154 pag.)WO2019/74809; (2019); A1;,
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