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SNAr (F)

[Aliphatic Amines (1o)]


Example 1

A solution of the aryl fluoride (A) (7.6 g, 35 mmol), the amine (B) (6 g, 35 mmol), and DIEA (13.5 g, 105 mmol) in EtOH (70 mL) was refluxed for 14 h. The mixture was then cooled to 20 C and the resulting precipitate was filtered and washed with EtOH to provide the product as an orange powder. [11 g, 94%]

[Patent Reference: WO2015158653, page 36, (2.9 MB)]