Simple exploration of 2-Fluoro-4-iodopyridine

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Each compound has different characteristics, and only by selecting the characteristics of the compound suitable for a specific situation can the compound be applied on a large scale. 22282-70-8, name is 2-Fluoro-4-iodopyridine. This compound has unique chemical properties. The synthetic route is as follows. Application In Synthesis of 2-Fluoro-4-iodopyridine

A solution of 401-A (21.6 g, 96.9 mmol) in 100 mL of dry THF was cooled to -70 C. The above LDA solutionwas added dropwise to the solution while the temperature was kept below -70 C. Then the solution was stirred at -70C for 1 hour. Ethyl formate (10 mL, 121 mmol) was added dropwise to the solution and slowly warmed to -50 C during1 hour. The reaction mixture was quenched with sat. NH4Cl and stirred at 25 C for 30 minute. THF was removed byevaporation and the reaction solution was extracted with EtOAc (300 mL2). The combined organic phase was washedwith water and brine, dried over Na2SO4. Na2SO4 was filtered and the organic phase was concentrated to dry and theresidue was purified by column chromatography on silica gel (PE/EtOAc: 50:1 to 10:1) to give the product 401-B (2-fluoro-4-iodonicotinaldehyde, 13.0 g, yield: 53%).1H NMR (300 MHz, DMSO-d6): delta 10.15 (s, 1H), 7.97 (d, J = 5.1 Hz, 1H), 7.87 (d, J = 5.1 Hz, 1H).

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Reference:
Patent; Kangpu Biopharmaceuticals, Ltd.; LEE, Wen-Cherng; LIAO, Baisong; ZHANG, Lei; EP3590924; (2020); A1;,
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