Natural Fluconazole raw Materials Powder Fluconazole

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Fluconazole Powder Usage and Synthesis.

1. Systemic candidiasis: including candidemia, disseminated candidiasis, and other forms of invasive candidiasis, such as peritoneal, endocardial, pulmonary, and urinary tract infections. It can also be used in patients with malignant tumors, special care patients, patients receiving radiotherapy, chemotherapy or immunosuppressive therapy, or other factors predisposed to candida infection. It can also be used to prevent candida infection when bone marrow transplant patients receive cytotoxic drugs or radiation therapy.

2, cryptococcal disease: including cryptococcal meningitis and other sites (such as lungs, skin) cryptococcal infection. It can be used for patients with normal immune function, AIDS patients and patients with organ transplantation or other reasons caused by immune function suppression. AIDS patients can take this product to maintain treatment to prevent the recurrence of cryptococcosis.

3, mucosal candidiasis: including oral and pharyngeal, esophageal, non-invasive bronchial mucosal candidiasis, pulmonary candidiasis, candidiuria, cutaneous mucous membranes and chronic atrophic oral candidiasis. It can be used in patients with normal or impaired immune function.

4. Fluconazole can also replace itraconazole in the treatment of blastomycosis and histoplasmosis.

5. Acute or recurrent vaginal candidiasis.

6, to receive chemotherapy or radiotherapy and prone to fungal infection of leukemia patients and other malignant tumor patients, the product can be used for preventive treatment.

7. Coccidioidomycosis.

8. Dermatomycosis: including tinea corporis, tinea handi, tinea pedis, tinea versicolor, tinea capitis, tinea digitalis and other skin fungal infections.

9, Fluconazole can be used for the treatment of skin pigmented mycosis.

Uses of Fluconazole.

Fluorotriazole broad-spectrum antifungal drugs, antibacterial spectrum and ketoconazole similar, long-term, deep infection fungal drugs effective, strong antifungal action, good oral absorption. It is mainly used for candidiasis and cryptococcosis, and is also effective against oropharyngeal candidiasis in cancer patients.

Pharmacological action of Fluconazole.

Fluconazole is a fluorotriazole antifungal drug, its antibacterial spectrum is similar to ketoconazole, and its antibacterial activity is stronger than ketoconazole. The mechanism of action is to inhibit ergosterol synthetase, which is an essential component of fungal cell membrane, to block ergosterol synthesis, destroy the integrity of fungal cell wall, and inhibit its growth and reproduction. This product has strong antibacterial activity against Candida albicans, microspora, Cryptococcus neoformans, epidermophyton and histoplasma capsulatus.

Product Method of Bulk Fluconazole Powder.

1H-1, 2, 4-triazole can be obtained by formamide, hydrazine hydrate and 85% formic acid. M-difluorobenzene is obtained from m-phenylenediamine, which is then brominated to 2, 4-difluorobromobenzene. Magnesium was dissolved in anhydrous ether, and an ether solution of 2, 4-difluorobromobenzene was added under ultrasonic radiation, and then an ether solution of 1, 3-dichloroacetone was added under ice bath cooling, and stirred at room temperature overnight. Add glacial acetic acid and water. The separated organic layer concentrates after drying. The concentrated solution, triazole, potassium carbonate and PEG600 were dissolved in dry ethyl acetate and refluxed. Strain, rinse until neutral and dry. Fluconazole was obtained by recrystallization of ethyl acetate monohexane (1:1) with a total yield of 33.6% and melting point of 138.5-140℃.

The last step can also be performed in propionitrile. Fluconazole was obtained by reflux of 1, 3-dihalide (x=Br or Cl)-2-(2, 4-difluorophenyl) -2-propanol and 1h-1, 2, 4-triazole in propionitrile, catalyzed by sodium hydroxide and catalyzed by PEG-600 phase transfer. The crude product is dissolved in fat alcohol (such as propyl alcohol, isopropyl alcohol or butanol, etc.), heated to dissolve, decolorized with a small amount of activated carbon, cooled to crystallize, that is, fluconazole fine, melting point 139 ~ 140℃.

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