Diethyl Sulfate → (6S-cis)-1-chloro-N-[2-chloro-4-fluoro-5-(6-fluorotetrahydro-1,3-dioxo-1H-pyrrolo[1,2-c]imidazol-2(3H)-yl)phenyl]-N-ethylmethanesulfonamide

関与物質

反応手順

A mixture of the title compound of Example 1, Step H (0.414 g, 1 mmol), diethylsulfate (0.17 g, 1.1 mmol), and potassium carbonate (0.27 g) in acetone (10 mL) was stirred at room temperature for 4 h. After completion of the reaction, the potassium carbonate was filtered off and the solvent was removed on a rotary evaporator. The title compound of Step A, a compound of this invention, was isolated by flash chromatography (0.41 g, 92%) as a white solid melting at 198-200° C. 1H NMR (CDCl3) δ 7.46 (d, 1H), 7.42 (d, 1H), 5.52 (m, 1H), 4.62 (dd, 1H), 4.59 (s, 2H), 4.02 (dd, 1H), 3.80 (m, 4H), 3.60 (dd, 1H), 2.64 (m, 1H), 2.01 (m, 1H), 1.20 (t, 6).

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