A Process for The Preparation Of 2,7-Dihydroxyfluorenone Useful for the Synthesis of Tilorone and its Salts

1. The method provides a simple strategy for synthesizing Tilorone from fluorene with high yield, simple reaction operation, low cost and less environmental pollution.
2. Subsequent product separation of this method uses filtration and crystallization methods, avoiding the existing methods that require a large amount of water washing and column separation, low yield and hazardous chemicals.
3. The new methodology is simple and feasible. It is not only suitable for small-scale laboratory preparation, but also suitable for large-scale production.

The invention relates to a method for the preparation of 2,7-dihydroxyfluorenone useful for the synthesis of tilorone and its salts selected from the group consisting of bromide, iodide, fluoride, citrate, oxalate, maleate, phosphate, tartrate, triflate, trifluoroacetate, tetrafluoroborate. More particularly, the invention relates to a method for the preparation of tilorone dihydrochloride salt which is an orally active interferon inducing agent.

The new methodology is simple and feasible. It is not only suitable for small-scale laboratory preparation, but also suitable for large-scale production.