Electric Literature of 105252-99-1, With the rapid development and complex challenges of chemical substances, the synthesis of new drugs is usually one of the most effective ways to increase yield.105252-99-1, name is 4-Amino-6-fluoropyridin-2(1H)-one, molecular formula is C5H5FN2O, molecular weight is 128.1, as common compound, the synthetic route is as follows.
Step a: To a 0 C solution of 4-amino-6-fluoropyridin-2(1H)-one (490 mg, 3.83 mmol) in AcOH (19 mL) was added NIS (818 mg, 3.63 mmol). The reaction mixture solidated, was allowed to warm to RT, and stirred for 1 h. The volatiles were removed under reduced pressure. The residue was transferred to a separation funnel containing sat. aq. Na25203 (15 mL), sat. aq. NH4C1 (15 mL), and water (15 mL). The mixture was extracted with Et20 (4 x 50 mL) and the combined organic extracts were dried over Mg504, filtered, and the volatiles were removed under reduced pressure. The residue was purified by silica chromatography (0 to 5% gradient of MeOH/DCM) to give 4-amino-6-fluoro-3-iodopyridin-2(1H)-one (54 mg, 0.2 13 mmol) as a white solid. MS m/z 255.0 (M+H).
The chemical industry reduces the impact on the environment during synthesis 105252-99-1, I believe this compound will play a more active role in future production and life.
Reference:
Patent; NOVARTIS AG; CHEN, Zhuoliang; FORTANET, Jorge Farcia; LAMARCHE, Matthew J.; SENDZIK, Martin; TAMEZ, JR., Victoriano; YU, Bing; (237 pag.)WO2016/203405; (2016); A1;,
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