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  (Process Chem)


  (Chem Dev)

Amine to Amide



Example 1

A mixture of the acid (A) (200 mg, 0.81 mmol), the amine (B) (120 mg, 1.0 mmol), and TEA (0.29 mL, 1.6 mmol) in DMF (4 mL) was treated with PyBOP (380 mg, 1.0 mmol). After 2 h, the reaction mixture was concentrated in vacuo, suspended in H2O (25 mL), and stirred at RT. After 16 h, the mixture was filtered and the filter cake was washed with ether (2 x 2 mL) to provide the product as a yellow solid. [260 mg, 91%]

[Patent Reference: WO2015105749, page 89, (11.4 MB)]