Hydrochloric Acid → Desloratadine

Participants

Reaction Steps

To a solution of 9.1 g (0.238 mol) of loratadine in 120 mL of dry chloroform, was added 7.5 mL of trimethylsilyl iodide. Then, the mixture was heated to 55°-60° C. under an argon atmosphere overnight. 30 mL of 0.5N HCl was added and the mixture was stirred for some time more. After basifying with NaOH, the resulting solution was extracted with chloroform (2-3 times). The organic phase was dried over sodium sulfate and the solvent was removed, to yield 12.89 g of a residue that was purified by crystallization in acetonitrile. 5.69 g of the desired product was obtained (yield: 77%).

Provenance & Evidence