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Publication No: CN118175999 [China] Application No: CN202280070984
Title: Process for the preparation of 2, 7-dihydroxy-9-fluorenone useful for the synthesis of telulone and its salts
Publication Date: 11-06-2024 File Date: 19-10-2022
Inventor(s): Prasuraman Jaisankar; Indubusan Deb; Pinazi Batachalji
IPC Classification: A61K 31/343, C07C 213/02, C07C 217/22
Abstract: The present invention provides a process for the preparation of 2, 7-dihydroxy-9-fluorenone building blocks for the synthesis of telulone dihydrochloride and other salts of telulone (bromide, iodide, fluoride, citrate, oxalate, maleate, phosphate, tartrate, triflate, trifluoroacetate, tetrafluoroborate). An efficient, safe, cost-effective process for preparing 2, 7-bis- [2- (diethylamino) ethoxy ] -fluorenone-9 and its various salts has been developed. The process involves oxidation of fluorene, nitration of fluorenone, followed by reduction and diazotization to form the key intermediate 2, 7-dihydroxy-9-fluorenone for the formation of 2, 7-bis- [2- (diethylamino) ethoxy ] -9-fluorenone-dihydrochloride (telulone dihydrochloride) and other telulone salts. The current synthesis method has the advantages of simpler operation, mild reaction conditions, high yield and simple process, and the yield is 80-97%. The subsequent purification of the product of this process utilizes filtration and crystallization methods, avoiding the existing column chromatography methods.
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Industrial Applications NCE [Drugs and Pharmaceuticals] Synhtesis Procesess [Drugs and Pharmaceuticals]