反应详情

A mixture of 4-bromo-7-hydroxy-2-phenyl-thiazolo[5,4-c]pyridine-6-carboxylic acid ethyl ester (191 mg, 0.50 mmole) and glycine (1.33 g, 17.69 mmole) in 0.5 M sodium methoxide/methanol (25.3 ml) was refluxed for 28 h before it was cooled to room temperature and concentrated in vacuo. The residue was dissolved in water (120 ml) and extracted with dichloromethane (3×100 ml). The remaining aqueous layer was acidified to pH=2 with 1N HCl. The resulting precipitate was filtered, washed with water and dried in vacuo to give the title compound as a yellow solid (137 mg). MS: (+) m/z 408.12, 410.09 (M+1, 79Br/8tBr), (−) m/z 406.08, 408.05 (M−1, 79Br/81Br).

1. temperaturewas refluxed for 28 h before it
2. concentrationconcentrated in vacuo
3. dissolutionThe residue was dissolved in water (120 ml)
4. extractionextracted with dichloromethane (3×100 ml)
5. filtrationThe resulting precipitate was filtered
6. washwashed with water
7. customdried in vacuo