Terbinafine base

Introduction Terbinafine hydrochloride can treat skin, hair and nail infections caused by Trichophyton, Microsporum canis and Epidermophyton floccosum. It can also treat various ringworms, skin yeast infections caused by Candida, and onychomycosis caused by fungi. Terbinafine hydrochloride is an allylamine antifungal drug that inhibits squalene epoxidase during the synthesis of ergosterol in fungal cells and causes squalene to accumulate in the cells to play a bactericidal effect. Purification method step 1 (synthesis of crude terbinafine hydrochloride): Add 12.5ml purified water and potassium carbonate (4.06g, 29.2mmol) to a 100ml three-neck reaction bottle, stir and dissolve, then add N-methylnaphthylamine (5.01 g, 29.2mmol), then add 1-chloro-6,6-dimethyl-2-heptene-4-yne (4.57g, 29.2mmol), raise the temperature to 80°C for reaction, and after 4 hours, cool to room temperature. Add 25 ml of ethyl acetate for extraction, separate the ethyl acetate phase and cool to 0-10°C. Add 6N hydrochloric acid aqueous solution dropwise, adjust the pH to 1, stir for 1-2 hours, filter, and dry the filter cake under vacuum at 70°C for 4 hours to obtain Crude terbinafine hydrochloride (8.51g, yield: 89%); Step 2 (Purification of crude terbinafine hydrochloride): Add crude terbinafine hydrochloride (8.51g, 26.8mmol) to the 2Chemicalbook 50ml single-neck bottle, 106 ml of purified water, heated and refluxed until dissolved, cooled to room temperature naturally, cooled to 0-10°C in ice bath, stirred for 1 hour, filtered, vacuum dried the filter cake at 70°C for 3 hours to obtain the finished product of terbinafine hydrochloride (7.66g, purity 99.988 %, yield 90%). Applicable for oral administration: ① Trichophyton caused by Trichophyton rubrum (Trichophyton rubrum, Trichophyton mentagrophytes, Trichophyton verrucosum, Trichophyton trichophyton, Trichophyton violaceum, etc.), Microsporum and Epidermophyton floccosum Infections of the skin, hair and fingernails. ② Various ringworms and skin yeast infections caused by Candida. ③Onychomycosis (onychomycosis infection) caused by mold. Chemical Properties: White crystals are used as allylamine antifungal drugs. They have a wider antibacterial spectrum than naftifen and have higher antifungal activity. It can highly selectively inhibit the squalene epoxidase of fungi, blocking the squalene epoxidation reaction during the formation of fungal cell membranes, destroying the formation of fungal cell membranes, and killing or inhibiting fungi. It is safe, has low toxicity, few side effects, is well tolerated for oral and external use, and has no teratogenicity or embryotoxicity. Clinically used for various skin fungal infections (tinea pedis, tinea cruris and tinea corporis) and nail fungal infections.
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Terbinafine hydrochloride can treat skin, hair and nail infections caused by Trichophyton, Microsporum canis and Epidermophyton floccosum. It can also treat various ringworms, skin yeast infections caused by Candida, Chemicalbook, and onychomycosis caused by fungi. Terbinafine hydrochloride is an allylamine antifungal drug that inhibits squalene epoxidase during the synthesis of ergosterol in fungal cells and causes squalene to accumulate in the cells to play a bactericidal effect.