反应详情

To tert-butyl 1-(2-hydroxy-2-(4-(5-(5-phenyl-4-propylisoxazol-3-yl)-1,2,4-oxadiazol-3-yl)phenyl)ethyl)azetidine-3-carboxylate (8 mg, 0.015 mmol) was added DCM (2 mL) and TFA (2.000 mL). The reaction mixture was stirred 2 hours. Next, the solvent was removed and the remaining contents were freeze dried from MeCN to yield 8 mg of 1-(2-hydroxy-2-(4-(5-(5-phenyl-4-propylisoxazol-3-yl)-1,2,4-oxadiazol-3-yl)phenyl)ethyl)azetidine-3-carboxylic acid as a TFA salt. 1H NMR (400 MHz, DMSO-d6) δ ppm 8.19 (2H, d, J=8.35 Hz), 7.83 (2H, dd, J=8.02, 1.65 Hz), 7.58-7.73 (5H, m), 4.32-4.83 (3H, m), 3.43-4.20 (6H, m), 2.95-3.05 (2H, m), 1.65-1.75 (2H, m), 0.97 (3H, t, J=7.36 Hz). MS (m+1)=475. HPLC Peak RT=3.38 minutes (Analytical Method A). Purity=90%.

1. customNext, the solvent was removed
2. dry with materialdried from MeCN