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温度

0 °C

To a solution of Cis-2-chloro-N-(−4-(hydroxymethyl)cyclohexyl)-5-(trifluoromethyl)-benzamide (1 g, 2.98 mmol) in DCM (18 mL) is added DIPEA (2.081 mL, 11.91 mmol). The reaction mixture is cooled to 0° C. and pyridine-sulfur trioxide (1.896 g, 11.91 mmol) in DMSO (6 mL) is added. The reaction mixture is stirred at this temperature for 30 mins. The reaction mixture is partitioned between water and DCM and passed through a phase separator. The DCM layer was collected and concentrated under reduced pressure to give a colourless oil. Purification by chromatography on a pre-packed silica gel column using 0-100% EtOAc in isohexane gradient elution gave the desired product as a colourless solid.

1. customThe reaction mixture is partitioned between water and DCM
2. customThe DCM layer was collected
3. concentrationconcentrated under reduced pressure
4. customto give a colourless oil
5. customPurification by chromatography on a pre-packed silica gel column
6. wash0-100% EtOAc in isohexane gradient elution