Reference of 501-00-8,Some common heterocyclic compound, 501-00-8, name is 2-(3-Fluorophenyl)acetonitrile, molecular formula is C8H6FN, 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 A. 3-Fluoro-phenyl-piperidin-4-ylidene-acetonitrile.; To a mixture of 3-fluoro-phenyl-acetonitrile (3.2 g, 24 mmol) and 4-oxo-piperidine-1-carboxylic acid tert-butyl ester (4.0 g, 20 mmol) in THF (100 mL) was added NaHMDS (1.0 M in THF, 24 mL). The mixture was stirred at rt for 16 h, then was diluted with MeOH (16 mL) and concentrated. The residue was diluted with TFA (40 mL) and stirred at rt for 16 h. The mixture was concentrated and the residue was diluted with satd. aq. NaHCO3 (160 mL) and extracted with EtOAc (3×80 mL). The combined organic layers were filtered and concentrated to provide the crude title compound.
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route 2-(3-Fluorophenyl)acetonitrile, its application will become more common.
Reference:
Patent; Bonaventure, Pascal; Carruthers, Nicholas I.; Chai, Wenying; Dvorak, Curt A.; Jablonowski, Jill A.; Rudolph, Dale A.; Seierstad, Mark; Shah, Chandravadan R.; Swanson, Devin M.; Wong, Victoria D.; US2007/100141; (2007); A1;,
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