667932-40-3

General procedure for the synthesis of 5-alkynyl-3-amines from 5-((trimethylsilyl)ethynyl)pyridin-3-amines: a mixture of 5.26 g (27.6 mmol) of 5-((trimethylsilyl)ethynyl)pyridin-3-amine (B-18) and 7.63 g (55.2 mmol) of potassium carbonate in 90 mL of methanol was stirred at room temperature for 30 min. Upon completion of the reaction, the solvent was removed by concentration under reduced pressure and the residue was dissolved in 50 mL of dichloromethane and extracted with 50 mL of water. The organic layer was separated and dried with anhydrous magnesium sulfate, followed by removal of the solvent under reduced pressure. The resulting crude product was used in the subsequent reaction without further purification. The yield was 3.15 g in 96% yield.

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