反应详情

A mixture of ethyl [5-(1H-tetrazol-1-yl)pyrazin-2-yl]acetate (2.0 g, 8.5 mmol) in 60 mL of THF/MeOH/H2O (2:2:1) was added LiOH.H2O (540 mg, 12.8 mmol) portionwise and stirred for 30 minutes before diluted with 200 mL of water and washed with ether (30 mL*3). The water layer was acidified to pH=4 with diluted hydrochloric acid and extracted with EtOAc (50 mL*5). The combined organic layer was washed with brine, dried over anhydrous Na2SO4 and concentrated to afford [5-(1H-tetrazol-1-yl)pyrazin-2-yl]acetic acid. 1H-NMR (400 MHz, d6-DMSO) δ ppm 12.93 (brs, 1H), 10.22 (s, 1H), 9.25 (d, J=1.2 Hz, 1H), 8.71 (d, J=1.2 Hz, 1H), 3.98 (s, 2H).

1. washwashed with ether (30 mL*3)
2. extractionextracted with EtOAc (50 mL*5)
3. washThe combined organic layer was washed with brine
4. dry with materialdried over anhydrous Na2SO4
5. concentrationconcentrated