反应详情

The 1-[3-benzoyloxy-5-(diethoxy-phosphorylmethoxy)-tetrahydrofuran-2-yl]-1H-[1,2,4]triazole-3-carboxylic acid methyl ester (60 mg. 0.124 mmol) was dissolved in MeCN (1.5 mL). Bromotrimethylsilane (0.164 mL, 1.24 mmol) and 2,6-lutidine (0.043 mL, 0.372 mmol) were added and the mixture stirred at ambient temperature for 10 h. The solvents were removed in vacuo and the product isolated by C-18 HPLC. To this was then added ammonia (7 N in MeOH, 4 mL) and the mixture stirred overnight. The title compound was isolated by C-18 HPLC. 1H NMR (300 MHz, D2O) ppm 8.65 (s, 1H), 5.95 (d, 1H, J=2.4 Hz), 5.49-5.52 (m, 1H), 4.81-4.89 (m, 1H), 3.47-3.70 (m, 2H), 2.27-2.32 (m, 2H). 31P NMR (121.4 MHz, D2O) ppm 15.0. LRMS (ESI) M-H C8H12N4O7P requires 307.0 Found 307.0.

1. customThe solvents were removed in vacuo
2. customthe product isolated by C-18 HPLC