Lithium iodide → HCID 22036173, compound

Participants

Reaction Steps

To 694 mg (1.67 mmol) of (4-fluoro-3-methoxy-benzyl)-(4-methanesulfonyl-phenyl)-(3-methanesulfonyl-propyl)-amine, prepared following the method of Example 5 but replacing 3-pyridinecarboxaldehyde with 4-fluoro-3-methoxybenxaldehyde, dissolved in 3 mL of 2,4,6-collidine was added 402 mg (3.01 mmol) lithium iodide. The mixture was heated to 150 degrees for 3 hrs, cooled to room temperature, and partitioned between ethyl acetate and 1 N HCl. Upon drying over magnesium sulfate and concentration, column chromatography, eluting with acetone/dichloromethane, provided 169 mg of 2-fluoro-5-{[(4-methanesulfonyl-phenyl)-(3-methanesulfonyl-propyl)-amino]-methyl}-phenol; (m+H)+=401.

Provenance & Evidence