Water → methyl 4,6-diamino-2-(1-(2-fluorobenzyl)-5-(thiazol-2-yl)-1H-1,2,4-triazol-3-yl)pyrimidin-5-ylcarbamate

Participants

Reaction Steps

To a suspension of 2-(1-(2-fluorobenzyl)-5-(thiazol-2-yl)-1H-1,2,4-triazol-3-yl)pyrimidin-4,5,6-triamine (I-57, 0.31 mmol) in pyridine (2.0 mL) at 0° C. was treated with methyl chloroformate (1 equiv). After 30 min, additional portions of methyl chloroformate (3 equiv) were added and the reaction was stirred for 3 h. The reaction mixture was poured into water and the resultant tan solid was collected by filtration to afford methyl 4,6-diamino-2-(1-(2-fluorobenzyl)-5-(thiazol-2-yl)-1H-1,2,4-triazol-3-yl)pyrimidin-5-ylcarbamate (74% yield).

Provenance & Evidence