Water → (2-chloro-11-fluoro-6H-pyrido[2',3':5,6][1,3]oxazino[3,4-a]indol-6-yl)methyl methanesulfonate

Participants

Reaction Steps

To a solution of (2-chloro-11-fluoro-6H-pyrido[2′,3′:5,6][1,3]oxazino[3,4-a]indol-6-yl)methanol (1.00 g, 3.29 mmol) in dry pyridine (10 mL) at room temperature was added dropwise MsCl (1.23 g, 10.74 mmol) at 0° C. Then the reaction mixture was stirred at room temperature for 2 hours under N2 protection. The reaction was poured into water and filtered. The filter cake was washed with water and dried to provide (2-chloro-11-fluoro-6H-pyrido[2′,3′:5,6][1,3]oxazino[3,4-a]indol-6-yl)methyl methanesulfonate (1.20 g, yield: 90.1%). 1H-NMR (DMSO-d6, 400 MHz) δ 7.37˜7.51 (m, 2H), 7.28˜7.33 (m, 2H), 7.18˜7.24 (d, J=8.4 Hz, 1H), 6.9-6.98 (m, 1H), 6.65˜6.72 (m, 1H), 4.46˜4.53 (m, 1H), 4.31˜4.38 (m, 1H), 2.90 (s, 3H). MS (M+H)+: 383.

Provenance & Evidence