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Open AccessCommunication
Molecules 2015, 20(12), 21458-21463;

An Effective Synthesis Method for Tilorone Dihydrochloride with Obvious IFN-α Inducing Activity

School of Chemical Engineering, Nanjing University of Science and Technology, Nanjing 210094, China
Laboratory of Veterinary Pharmacology and Toxicology, College of Veterinary Medicine, Nanjing Agricultural University, Nanjing 210095, China
School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China
These authors contributed equally to this work.
Author to whom correspondence should be addressed.
Academic Editor: Maria Emília de Sousa
Received: 9 October 2015 / Revised: 18 November 2015 / Accepted: 26 November 2015 / Published: 2 December 2015
(This article belongs to the Section Medicinal Chemistry)
Full-Text   |   PDF [805 KB, uploaded 2 December 2015]   |  


Tilorone dihydrochloride (1) has great potential for inducing interferon against pathogenic infection. In this paper, we describe a convenient preparation method for 2,7-dihydroxyfluoren-9-one (2), which is a usual pharmaceutical intermediate for preparing tilorone dihydrochloride (1). In the novel method, methyl esterification of 4,4′-dihydroxy-[1,1′-biphenyl]-2-carboxylic acid (4) was carried out under milder conditions with higher yield and played an important role in the preparation of compound 2. The structures of the relative intermediates and target compound were characterized by melting point, IR, MS, and 1H-NMR. Furthermore, the synthesized tilorone dihydrochloride exhibited an obvious effect on induction of interferon-α (IFN-α) in mice within 12 h, and the peak level was observed until 24 h. This fruitful work has resulted in tilorone dihydrochloride becoming available in large-scale and wide application in clinics, which has a good pharmaceutical development prospects. View Full-Text
Keywords: synthesis; 2,7-dihydroxyfluoren-9-one; tilorone; methyl esterification; IFN-α synthesis; 2,7-dihydroxyfluoren-9-one; tilorone; methyl esterification; IFN-α

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Zhang, J.; Yao, Q.; Liu, Z. An Effective Synthesis Method for Tilorone Dihydrochloride with Obvious IFN-α Inducing Activity. Molecules 2015, 20, 21458-21463.

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