Synthesis
b) Synthesis of 5-fluorothiazol-2-amine hydrochloride; N-(5-fluoro-2-thiazolyl)-carbamic acid-1,1-dimethylethyl ester (4.6 g, 21.1 mmol) was dissolved in dioxane (25 mL). HCl gas was passed into the solution for 4 h. Subsequently, ether (50 mL) was added to form a suspension and the solid was collected by filtration. The resulting solid was dried under high vacuum to give 5-fluorothiazol-2-amine hydrochloride (3.03 g, 19.7 mmol, 93% yield). The product was confirmed by 1H NMR (D2O): δ 7.00 (1H, d); mass spectrometry analysis showed m/z = 119.0 [M + H]+.
References
[1] Organic Process Research and Development, 2006, vol. 10, # 2, p. 346 - 348
[2] Patent: WO2006/16178, 2006, A1. Location in patent: Page/Page column 9
[3] Patent: WO2006/16174, 2006, A1. Location in patent: Page/Page column 17
[4] Patent: EP2105435, 2009, A1. Location in patent: Page/Page column 54-55
[5] Patent: WO2012/51450, 2012, A1. Location in patent: Page/Page column 28
