OXAZOLE-2-CARBOXYLIC ACID AMIDE

Synthesis

General procedure for the synthesis of 1,3-oxazole-2-carboxamide from ethyl 1,3-oxazole-2-carboxylate: Example 111: Synthesis of 1,3-oxazole-2-carboxamide; Concentrated ammonium hydroxide (30 mL) was added to ethyl 1,3-oxazole-2-carboxylate (1.5 g, 10.6 mmol). The reaction mixture formed a turbid suspension which was converted to a white slurry by stirring overnight. The white solid product (0.98 g, 82% yield) was collected by filtration. The structure of the product was confirmed by 1H NMR (400 MHz, DMSO-d6): δ 8.28 (s, 1H), 8.21 (br.s, 1H), 7.87 (br.s, 1H), 7.42 (s, 1H).

References

[1] Patent: WO2006/43145, 2006, A1. Location in patent: Page/Page column 131
[2] Patent: WO2010/45009, 2010, A1. Location in patent: Page/Page column 40
[3] Patent: WO2010/45015, 2010, A1. Location in patent: Page/Page column 27
[4] Patent: WO2010/45016, 2010, A1. Location in patent: Page/Page column 19