High Purity Bulk Fluconazole Powder

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Fluconazole Powder Usage and Synthesis.

1, Systemic Candidiasis:Including candidaemia, disseminated candidiasis and other forms of invasive Candida infections, such as peritoneal, endocardial, pulmonary and urinary tract infections.

It may also be used in patients with malignant tumours, in special care patients, in patients receiving radiotherapy, chemotherapy or immunosuppressive therapy, or subjected to other factors predisposing them to Candida infections.

Can also be used for bone marrow transplant patients to receive cytotoxic drugs or radiation therapy, to prevent the occurrence of Candida infection.

2, cryptococcosis: including cryptococcal meningitis and other parts of the cryptococcal infection (such as lungs, skin).

It can be used for patients with normal immune function, AIDS patients and patients with organ transplantation or other causes of immune function suppression.

AIDS patients can take this product for maintenance therapy to prevent recurrence of cryptococcosis.

3、Mucosal candidiasis:Including oropharynx, oesophagus, non-invasive bronchial and other mucosal candidiasis, pulmonary candida infections, candiduria, skin and mucous membranes and chronic atrophic oral candidiasis.

It can be used in patients with normal or impaired immune function.

Fluconazole can also be used as an alternative to itraconazole in the treatment of budding mycosis and histoplasmosis.5. Acute or recurrent vaginal candidiasis.

6, to accept chemotherapy or radiotherapy and prone to fungal infections in patients with leukaemia and other malignant tumours, can be used for preventive treatment.

7、Coccidioidomycosis.

8、Skin fungal diseases:including tinea corporis,tinea cruris,tinea pedis,tinea pedis,tinea cruris,tinea capitis,tinea pedis and other skin fungal infections.

9、Fluconazole can be used in the treatment of skin colouring fungal disease.

Uses and functions of Fluconazole .

Fluorotriazoles broad-spectrum antifungal drugs, antimicrobial spectrum and ketoconazole similar, long-lasting, effective in deep infections fungal drugs, strong antifungal effect, oral absorption is good. It is mainly used for candidiasis and cryptococcosis, and is also effective for oropharyngeal candida infections in cancer patients.

Pharmacological Effects of  Fluconazole.

Fluconazole is a fluorotriazole antifungal drug, the antibacterial spectrum is similar to ketoconazole, antibacterial activity is stronger than ketoconazole.

Its mechanism of action is to inhibit the essential component of fungal cell membrane ergosterol synthase, so that ergosterol synthesis is blocked, destroying the integrity of the fungal cell wall and inhibiting its growth and reproduction.

Fluconazole on Candida albicans, large and small spores, new cryptococcus, epidermolysis bullosa and podoconiosis cytoplasmic bacteria have strong antibacterial activity.

Production method of  Bulk Fluconazole Powder.

Method 1: 1H-1,2,4-triazole is obtained from formamide, hydrazine hydrate and 85 per cent formic acid. From m-phenylenediamine, m-difluorobenzene is obtained, which is then brominated to give 2,4-difluorobromobenzene.

Magnesium is dissolved in anhydrous ether, and an ether solution of 2,4-difluorobromobenzene is added dropwise under ultrasonic radiation, then an ether solution of 1,3-dichloroacetone is added dropwise under cooling in an ice bath and stirred at room temperature overnight. Glacial acetic acid and water were added.

The separated organic layer was dried and concentrated. The concentrate and triazole, potassium carbonate and PEG600 were dissolved in dry ethyl acetate and refluxed. Filtered, washed with water to neutral and dried. The solvent was evaporated and ethyl acetate a cyclohexane (1:1) was recrystallised to give fluconazole in a total yield of 33.6%, melting point 138.5-140°C.

The last step can also be carried out in propionitrile. 1,3-dihalogen (x=Br or Cl-2-(2,4-difluorophenyl)-2-propanol and 1H-1,2,4-triazole in propionitrile, sodium hydroxide-catalysed and PEG600 phase-transfer-catalysed refluxing, the crude product of fluconazole can be obtained.

The crude product is dissolved in fatty alcohols (such as propanol, isopropanol or butanol, etc.), heated to dissolve, decolourised with a small amount of activated charcoal, and then cooled to obtain crystals, i.e. fluconazole bouquets with a melting point of 139-140 ℃.

Method 2:Methyl 2,4-difluorobenzoate and 1-chloromethyl-1,2,4-triazole reaction of Grignard reagent and hydrolysis can be obtained fluconazole.

Method 3: Difluorobenzene is brominated to produce 1-bromo-2,4-difluorobenzene, which is then converted to its Grignard reagent. The Grignard reagent obtained above is reacted with 1,3-bis(1H-1,2,4-triazolyl)acetone and hydrolysed to obtain fluconazole.

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