Sodium Nitrite → 1,1-dimethylethyl (2S)-2-(3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-ylmethyl)-1-pyrrolidinecarboxylate

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Reaction Steps

1,1-Dimethylethyl (2S)-2-{[(5-amino-4-pyrimidinyl)amino]methyl}-1-pyrrolidinecarboxylate (1.6633 g, 5.67 mmol) and sodium nitrite (469 mg, 6.80 mmol) were dissolved in a mixture of acetic acid (5 mL) and water (8 mL), and the mixture was stirred vigorously for 1 h. The solution was concentrated in vacuo to provide 1,1-dimethylethyl (2S)-2-(3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-ylmethyl)-1-pyrrolidinecarboxylate (1.98 g, >99%). LCMS: (M+H)+: 305.2.

Provenance & Evidence