Trifluoroacetic acid → Ethyl 5-(aminomethyl)-3-isoxazolecarboxylate

Participants

Reaction Steps

Trifluoroacetic acid (2.1 ml, 29 mmol) was added to a solution of 3-ethoxycarbonyl-5-[N-(tert-butyloxycarbonyl)aminomethyl]isoxazole (Method 73; 790 mg, 2.9 mmol) in DCM (15 ml). The mixture was stirred at ambient temperature for 4 hours then the volatiles removed by evaporation. The residue was triturated with diethyl ether to give the title compound (763 g, 93%). NMR (DMSO): 1.31 (t, 3H), 4.37 (m, 2H), 6.97 (s, 1H), 8.64 (s, 3H); m/z 171 (MH)+.

Provenance & Evidence