Pharmaceutical intermediates Terbinafine Hydrochloride CAS 78628-80-5Pharmaceutical intermediates Te

CAS:78628-80-5

MF: C21H26ClN

MW:327.89

EINECS:616-640-4

Specification: 99% min Terbinafine Hydrochloride

Sample:Terbinafine Hydrochloride Powder

Packaging:1kg/bag, 25kg/drum

Brand: Henrikang

Appearance:White

Storage: Cool Dry Place

Shelf Life: 2 Years

Test Method: HPLC

Terbinafine Hydrochloride Usage and Synthesis.

Terbinafine hydrochloride is an acrylamide-based broad-spectrum antifungal drug for dermatological use. Currently, it is sold in more than 90 countries around the world.

It can specifically disturb the late biological decomposition of fungal sterols, selectively inhibit the activity of squalene epoxidase of fungi, and block the squalene epoxidation reaction in the process of fungal cell membrane constitution, so as to achieve the effect of killing or inhibiting fungi.

It is suitable for the treatment of skin candidiasis, such as tinea cruris, tinea pedis, tinea cruris, tinea corporis and tinea pedis, and it is also the best medicine for the treatment of grey nails.

Terbinafine Hydrochloride entered the first batch of OTC catalogue announced by the state in 2000.

This product belongs to the antifungal class of drugs, it has a strong effect on superficial fungal infections, topical application can cure most of the skin fungal diseases.

Uses and functions of Terbinafine Hydrochloride.

Terbinafine hydrochloride is an acrylamide with broad-spectrum antifungal activity, which has significant efficacy in foot fungus, grey nails, ringworm, jock itch, tinea pedis, etc., caused by fungi, and can also be used in bronchial asthma, wheezing bronchitis and emphysema.

1. Skin, hair and nail infections caused by Trichophyton (Trichophyton albicans, Trichophyton mustelii, Trichophyton verrucosum, Trichophyton vulgaris and Trichophyton purpureum, etc.), Microsporum canis and Floccus epidermidis.

2. All kinds of ringworm (tinea corporis, tinea cruris, tinea pedis and tinea capitis, etc.) and skin yeast infections caused by Candida (Candida albicans, etc.).

3. Ringworm of the nails (nail fungal infections) caused by moulds.

Adverse Reaction of Terbinafine Hydrochloride.

Terbinafine hydrochloride is mainly associated with two types of gastrointestinal and cutaneous adverse reactions, with an incidence of 4.9% and 2.3%, respectively, while other rare adverse reactions include loss of taste, hepatic abnormalities, visual abnormalities, neutropenia, and neurological adverse reactions including headache, dizziness, vertigo, and sensory abnormalities.

Oral terbinafine has been reported to cause fixed-type drug rash, erythema multiforme, urticaria-like and eczema-like rashes, acute generalised eruptive pustulosis, pruritus, and pemphigus vulgaris, etc., especially oral terbinafine caused acute generalised eruptive pustulosis.

Throughout the domestic and international reports on adverse reactions, almost all of them are caused by oral terbinafine hydrochloride, and there are fewer reports of adverse reactions caused by topical terbinafine hydrochloride.

Numerous studies have been conducted by scholars at home and abroad on the possibility of more serious adverse reactions to oral terbinafine hydrochloride.

Studies have shown that oral terbinafine hydrochloride causes more serious adverse reactions of liver damage, however, the incidence of liver damage caused by terbinafine hydrochloride is lower.

Synthetics method of Bulk Terbinafine Hydrochloride.

1.Synthesis of crude terbinafine hydrochloride:

To a 100 ml three-necked reaction flask was added 12.5 ml of purified water, potassium carbonate (4.06 g, 29.2 mmol), stirred to dissolve and then added N-methylnaphthalenemethylamine (5.01 g, 29.2 mmol), and then added 1-chloro-6,6-dimethyl-2-hepten-4-ynes (4.57 g, 29.2 mmol), the reaction was heated up to 80 ℃ for 4 h. After Cooled to room temperature, add 25ml ethyl acetate extraction, separated from the ethyl acetate phase and cooled to 0-10 ℃, dropwise addition of 6N aqueous hydrochloric acid, adjust the pH to 1, stirring 1-2h, filtration, filter cake at 70 ℃ in a vacuum drying 4h to get the crude terbinafine hydrochloride (8.51g, yield: 89%);

2.Purification of terbinafine hydrochloride crude product:

To 250ml single-necked bottle add terbinafine hydrochloride crude (8.51g, 26.8mmol), 106ml of purified water, heating reflux to dissolve clear, natural cooling to room temperature, ice bath cooling to 0-10 ℃, stirring for 1h, filtration, filter cake at 70 ℃ vacuum drying for 3h to get terbinafine hydrochloride finished product (7.66g, purity of 99.988%, yield 90%).