Electric Literature of 3939-09-1,Some common heterocyclic compound, 3939-09-1, name is 2,4-Difluorobenzonitrile, molecular formula is C7H3F2N, 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 1: To a 0 C. solution of LiHMDS (360 mL, 359.5 mmol) in 148 THF (200 mL) was added drop wise, 439 2,4-difluorobenzonitrile (20 g, 143.8 mmol) in THF (100 mL). The reaction was warmed to rt and stirred for 4 hrs and c.HCl (100 mL) was added drop wise to keep the temperature below 30 C. 81 EtOAc was added and the aqueous layer was collected. The pH was adjusted to 10 by the careful addition of 6N 344 NaOH and the organic layer collected, dried and evaporated to dryness to give 440 2,4-difluoro benzimidamide (10 g, 44%) which was used without further purification in Step 2.
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 2,4-Difluorobenzonitrile, its application will become more common.
Reference:
Patent; CYSTIC FIBROSIS FOUNDATION THERAPEUTICS, INC.; Strohbach, Joseph Walter; Limburg, David Christopher; Mathias, John Paul; Thorarensen, Atli; Denny, Rajiah Aldrin; Zapf, Christoph Wolfgang; Elbaum, Daniel; Gavrin, Lori Krim; Efremov, Ivan Viktorovich; (159 pag.)US2018/141954; (2018); A1;,
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