(Diethylamino)sulfur trifluoride → HCID 71495924, compound

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Reaction Steps

To a stirred solution of 2-chloro-4-((3S,3aS,4S)-3-(2-fluoroethoxy)-4-hydroxy-3a,4,5,6-tetrahydro-3H-pyrrolo[1,2-b]pyrazol-2-yl)-3-methylbenzonitrile obtained in example 16 (120 mg, 0.36 mmol) in DCM (5 mL) at 0° C. was added DAST (0.05 mL, 0.43 mmol) and stirred at room temperature for 14 h. Once the starting material had disappeared (monitored by TLC) reaction mixture was diluted with DCM, water and extracted. Organic layer was washed with water, brine, dried over Na2SO4 and concentrated. Purification by column chromatography (silica gel, 50% EtOAc in Hexane) provided the title compound (60 mg, 50%).

Provenance & Evidence