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SNAr (F)

(Aliphatic Thiols)


Example 1

To a vial containing the aryl fluoride (B) (0.072 g, 0.2 mmol) was added DMSO (1.33 mL), Cs2CO3 (0.143 g, 0.440 mmol), and the thiol (A) (0.043 mL, 0.300 mmol). The reaction mixture was stirred at 100 C overnight. After cooling to RT, the mixture was filtered and purified by Prep HPLC (0.1% NH4OH in ACN/H2O) to provide the product. [33 mg, 31%]

[Patent Reference: WO2015051043, page 79, (9.7 MB)]