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The principle of the synthesis of Itraconazole

Abstract:
Itraconazole is a drug which was discovered in 1979 by J. Heeres and L.J.J. Backx of Janssen Pharmaceutica N.V. They were synthesizing new series of triazoles to test in vitro and in vivo. The results of the new antifungal agent, Itraconazole, proved to have a distinct oral activity role against fungi.
This synthetic antifungal agent has a molecular formula of C35H38Cl2N8O4(s), resulting in a molecular weight of 705.64 g/mol with a white to slightly yellow powder color. It is poorly soluble in water slightly soluble in alcohol, and very soluble in dichloromethane, as described by Janssen Pharmaceutica instruction leaflet of Sporanox, the marketed product of Itraconazole.

The objective of this research is to explain the synthesis route of Itraconazole for the students of Fontys University of Applied Sciences and describe it�s function (mean function of antifungal drugs). The synthesis process of itraconazole is first to synthesize ketoconazole, which is one of the first triazole antifungal agents.

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