[CH3:1][CH2:2][O:3][C:4]([C:6]1[N:10]=[C:9]([CH:11]2[CH2:16][CH2:15][NH:14][CH2:13][CH2:12]2)[O:8][CH:7]=1)=[O:5].C(N(CC)CC)C.[CH3:24][S:25](Cl)(=[O:27])=[O:26].O>C(Cl)Cl>[CH3:24][S:25]([N:14]1[CH2:15][CH2:16][CH:11]([C:9]2[O:8][CH:7]=[C:6]([C:4]([O:3][CH2:2][CH3:1])=[O:5])[N:10]=2)[CH2:12][CH2:13]1)(=[O:27])=[O:26]
Ethyl 2-(4-piperidino)-1,3-oxazole-4-carboxylate (500 mg, 2.230 mmol) and triethylamine (0.466 ml, 3.34 mmol) were dissolved in dry DCM and cooled down to 0° C. Methanesulfonyl chloride (0.190 ml, 2.453 mmol) was added slowly at 0° C. and the reaction mixture was stirred at RT overnight. Small amount of water was added carefully and organic phase was washed with 1M Na2CO3 and water. Organic phase was dried and evaporated to yield the title compound 89%. 1H-NMR (400 MHz; CDCl3): δ 1.38 (t, 3H), 1.97-2.11 (m, 2H), 2.15-2.24 (m, 2H), 2.81 (s, 3H), 2.88-3.07 (m, 3H), 3.72-3.82 (m, 2H), 4.39 (q, 2H), 8.17 (s, 1H).
Wird geladen…
