New downstream synthetic route of 2-Chloro-4-fluoropyridine

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,34941-91-8, its application will become more common.

Reference of 34941-91-8, In the chemical reaction process,reaction time,type of solvent,can easily affect the result of the reaction, thereby determining the yield and properties of the reaction product.An updated downstream synthesis route of 34941-91-8 as follows.

Step A: 2-Chloro-4-i uoropyridine~3~carboxylic acid (64-2)A solution of LDA (97 ml, 1.8 M heptane/THF/ethylbenzene, 175 mmol) and THF (304 ml) were combined and cooled to -78C. 2-Chloro-4-fluoropyridine (20.0 g, 152 mmol) was dissolved in 50 ml THF and then added dropwise over 20 minutes and then the solution was stirred for 1 hour. The reaction was poured onto dry ice and -the dry ice was allowed to evaporate. Water and 1 N NaOH were added to the residue. The mixture was extracted with Et20 and the organic layer discarded. The aqueous was acidified with 1 N HC1 and then extracted with EtOAc. The organic portion was washed with brine, dried (MgS04) and concentrated to give 64^2 (19 g, 71.2%) as an orange solid. MS (ESI): m/z = 176.0 (MH+).

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,34941-91-8, its application will become more common.

Reference:
Patent; MERCK SHARP & DOHME CORP.; BUNGARD, Christopher, James; PERKINS, James, J.; MANIKOWSKI, Jesse, J.; DE LEON, Pablo; MEISSNER, Robert, S.; WO2011/53574; (2011); A1;,
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