Diisopropylethylamine → 3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(1-(diphenylmethyl)azetidin-3-yl)-1H-1,2,3-triazol-4-yl)-2-aminopyridine

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Reaction Steps

The compound 3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-ethynyl-2-aminopyridine (4.2 g, 12.62 mmol) was dissolved in methanol (40 mL), and diisopropylethylamine (8.36 g, 64.78 mmol), copper iodide (62 mg, 0.33 mmol) and 1-(diphenylmethyl)-3-azidoazetidine (3.34 g, 12.62 mmol) were added successively. The reaction was stirred overnight at room temperature. TLC test showed that the raw materials were completely reacted. The resultant mixture was concentrated under reduced pressure;

Provenance & Evidence