反应详情

4-{4-[5-(2-Amino-pyrimidin-5-yl)-imidazo[2,1-b][1,3,4]thiadiazol-2-yl]-2-methoxy-phenoxy}-piperidine-1-carboxylic acid tert-butyl ester (9 mg; 0.017 mmol; 1 eq) was dissolved in anhydrous DCM (1 mL) and 4M HCl in 1,4-dioxane (0.042 ml, 0.17 mmol, 10 eq) was added. The reaction mixture was stirred at RT overnight. The solvent was evaporated and the residue was co-evaporated with DCM (×3). The residue was triturated in CH3CN and filtered. The oily-solid obtained was dissolved in MeOH and evaporated to give the desired product as HCl salt (6 mg, 77%). HPLC-MS (5-100% B in 8 min at 0.8 mL): tR=3.29 min, [M+H]+ m/z 424.1; 1H NMR (300 MHz, DMSO) δ 8.93 (s, 3H), 7.77 (s, 1H), 7.55 (m, 2H), 7.29 (d, J=8.9 Hz, 1H), 4.76 (m, 1H), 3.92 (s, 3H), 3.23 (m, 2H), 3.09 (m, 2H), 2.11 (m, 2H), 1.90 (m, 2H).

1. customThe solvent was evaporated
2. customThe residue was triturated in CH3CN
3. filtrationfiltered
4. customThe oily-solid obtained
5. customevaporated