Optimization of Fluconazol Synthesis: An Important Azole Antifungal Drug

Fluconazole is an azolic second-generation antifungal drug and is part of the National List of Essential Drugs (RENAME) of the Brazilian Ministry of Health. It is considered as first choice for the treatment of some opportunistic fungal infections and also applied in the AIDS treatment program as prophylactic therapy to avoid these infections. Due to the importance of fluconazole for the Brazilian Health System (SUS), it is strategic the domain of its obtaining process. Thus, improvements in the synthesis of this substance are also of special interest. In this work, many changes were proposed and carried out in the original fluconazole synthetic route, aiming to increase yield and using solvents and processes with a lower environmental impact. With these optimizations, the overall yield achieved was 53%, which is about 10 times higher than that of the original process.