New Invention Profile
| Publication No: | AU2022369156 [Australia] | Application No: | AU2022369156 |
| Title: | A process for the preparation of 2,7-dihydroxy-9-fluorenone useful for the synthesis of tilorone and its salts | ||
| Publication Date: | 09-05-2024 | File Date: | 19-10-2022 |
| Inventor(s): | Jaisankar Parasuraman; Deb Indubhusan; Bhattacharjee Pinaki | ||
| IPC Classification: | A61K 31/343, C07C 213/02, C07C 217/22 | ||
| Abstract: | The present invention provides a method for the preparation of building blocks of 2,7-dihydroxy-9-fluorenone towards the synthesis of tilorone dihydrochloride salt and other salts (bromide, iodide, fluoride, citrate, oxalate, maleate, phosphate, tartrate, triflate, trifluoroacetate, tetrafluoroborate) of Tilorone. An efficient, safe, cost effective method for the preparation of 2,7-bis-[2-(diethylamino)ethoxy]-fluorenone-9 and its various salts is developed. Method involves oxygenation of fluorene, nitration of fluorenone followed by reduction and diazotization towards the formation of 2,7-dihydroxy-9-fluorenone which is the key intermediate for the formation of 2,7-bis-[2-(diethylamino)ethoxy]- 9- fluorenone- dihydrochloride (Tilorone dihydrochloride) and other tilorone salts. The current synthesis method of the invention has relatively simple operation, mild reaction conditions, high yield and simple process with, yield 80-97%. Subsequent product purification of this method uses filtration and crystallization methods, avoiding the existing methods of column chromatography. |
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