Meloxicam Impurity 1 HCl synthesis

Yield:929568-25-2 100%

Reaction Conditions:

with hydrogenchloride;water in methanol at 120; for 1 h;Irradiation;

Steps:

32

3,4-difluoro-N-(5-methyloxazol-2-yl)benzamide (lOOmg, 0.42mmol) was dissolved in methanol (2ml) and water (1.5ml) and concentrated hydrochloric acid (1.5ml) were added. The mixture was heated at 12O⁰C in a sealed vessel under microwave irradiation for 1 hour. EPO The solution was diluted with water (70ml) and extracted with diethyl ether (2 x 70ml). The extracts were combined washed with 2N hydrochloric acid (60ml). All aqueous washings were combined, the solvent was removed by evaporation and the residue dried under vacuum to give 2-amino-4-methyloxazole hydrochloride (57 mg, 100%); NMR (400.13 MHz) 2.19 (3H, s), 7.02 (IH, s), 2.19 (3H, s), 9.13 (2H, s).

References:

WO2007/31745,2007,A1 Location in patent:Page/Page column 107-108