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Fenticonazole nitrate

Product Name
Fenticonazole nitrate
CAS No.
73151-29-8
Chemical Name
Fenticonazole nitrate
Synonyms
1-[2-(2,4-dichlorophenyl)-2-[[4-(phenylthio)phenyl]methoxy]ethyl]-1H-imidazole,nitrate (1:1);Falvin;Lomexin;Fentigyn;Fentiderm;Rec-15—1476;Fenticonazol Nitrate;FENTICONAZOLE NITRATE;FenticonazoleNitrate>Fenticonazole Nitrate EP
CBNumber
CB8481997
Molecular Formula
C24H21Cl2N3O4S
Formula Weight
518.41
MOL File
73151-29-8.mol
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Fenticonazole nitrate Property

Melting point:
135-137°C
storage temp. 
Inert atmosphere,Room Temperature
solubility 
Practically insoluble in water, freely soluble in dimethylformamide and in methanol, sparingly soluble in anhydrous ethanol
pka
6.54(at 25℃)
form 
Solid
color 
White to Pale Yellow
Merck 
14,4005
InChIKey
FJNRUWDGCVDXLU-UHFFFAOYSA-N
CAS DataBase Reference
73151-29-8(CAS DataBase Reference)
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Safety

RTECS 
NI4780000
HS Code 
2933.29.4300
Toxicity
LD50 in mice, male rats, female rats (mg/kg): 1191, 440, 309 i.p.; all >3000 orally (Graziani)
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
F0060000
Product name
Fenticonazole nitrate
Purity
European Pharmacopoeia (EP) Reference Standard
Packaging
f0060000
Price
$150
Updated
2024/03/01
TCI Chemical
Product number
F1008
Product name
Fenticonazole Nitrate
Purity
>97.0%(HPLC)
Packaging
200mg
Price
$124
Updated
2024/03/01
Cayman Chemical
Product number
29002
Product name
Fenticonazole (nitrate)
Packaging
50mg
Price
$70
Updated
2024/03/01
Cayman Chemical
Product number
29002
Product name
Fenticonazole (nitrate)
Packaging
100mg
Price
$93
Updated
2024/03/01
Cayman Chemical
Product number
29002
Product name
Fenticonazole (nitrate)
Packaging
10mg
Price
$32
Updated
2024/03/01
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Fenticonazole nitrate Chemical Properties,Usage,Production

Description

Fenticonazole nitrate is an antifungal imidazole derivative reported to be more effective than other imidazole antifungals such as miconazole, clotrimazole and econazole. In addition to its potent, broad-spectrum fungicidal activity, fenticonazole is also active against some Gram-positive bacteria.

Description

Fenticonazole is an imidazole with antimicrobial activity. It is active against clinical isolates of Candida species, including C. albicans, C. parapsilosis, C. tropicalis, C. krusei, and C. guilliermondii with MIC values ranging from 0.12 to 32 μg/ml. It is also active against clinical isolates of bacteria, including B. fragilis, associated with bacterial vaginosis (MICs = ≤0.03-16 μg/ml), as well as bacteria, including S. aureus and S. epidermidis, associated with skin infections with MIC values ranging from 0.03 μg/ml or less to greater than 16 μg/ml. Fenticonazole inhibits fungal growth in a guinea pig model of experimental M. canis dermatomycosis (ED50 = 0.5%, applied topically).

Chemical Properties

Off-White Solid

Originator

Recordati (Italy)

Uses

Broad spectrum antimycotic; also active as antibacterial. Antifungal (topical).

Definition

ChEBI: A racemate comprising equimolar amounts of (R)- and (S)-fenticonazole nitrate. Used for the treatment of vaginal candidiasis.

Manufacturing Process

1-(2',4'-Dichlorophenyl)-2-chloroethanol:
49.5 g of sodium borohydride were added slowly and in small parts to a suspension of 233 g of 1-(1'-hydroxy-2'-chloroethyl)-2,4-dichlorobenzene in 1 liter of methanol stirred at room temperature. The solution thus obtained was stirred at room temperature for a further two hours, and it was then poured into 1 liter of 5 N hydrochloric acid cooled with ice. After extraction with ethyl acetate or chloroform, the extract was washed with water, with 1 N sodium hydroxide, then again with water until neutrality, and finally with a saturated sodium chloride solution. The extract was dried, the solvent evaporated off and 220 g of an oil were obtained. The oil solidified on standing and the solid 1-(2',4'-dichlorophenyl)-2-chloro-ethanol melted at 48-51°C.
1-(2',4'-Dichlorophenyl)-2-(N-imidazolyl)ethanol:
30 g of sodium were added to a solution of 88.5 g of imidazole in 600 ml of methanol; the solvent was then evaporated off. The residue was dissolved in 300 ml of dimethylformamide and heated to 115-120°C. To the solution so obtained was added, dropwise and under stirring, a solution of 225 g of 1- (2',4'-dichlorophenyl)-2-chloroethanol in 400 ml of dimethylformamide. The mixture was heated to 115-120°C and maintained at that temperature for 20 min and, after subsequent cooling to 40°C, 2500 ml of iced water were added under vigorous stirring. The product precipitated under stirring over a period of about two hours, the upper liquid was then decanted off, a further 2500 ml of water were added and, after standing, the whole was filtered. The precipitate thus obtained was dried and crystallized from toluene. 170 g of the 1-(2',4'-dichlorophenyl)-2-(N-imidazolyl)ethanol, melting at 134-135°C, was obtained.
METHOD 1:
A solution of 2.57 g of 1-(2',4'-dichlorophenyl)-2-(N-imidazolyl)ethanol in 10 ml of hexamethylphosphoramide was dropped at 25°C into a suspension of 0.52 g of sodium hydride (50% in oil) in 5 ml of hexamethylphosphoramide. When hydrogen emission was over, the salification was completed by heating for 1 hour at 50°C. After cooling to 25°C, 2.58 g of 1-chloromethyl-4- phenylthiobenzene were added. The temperature was raised to 50°C and maintained at that temperature for 12 hours. At the end of the reaction, the mixture was poured into 200 ml of water, the product was extracted with diethyl ether, the solvent was evaporated off and the residue was purified twice on a silica gel column, using ethyl acetate as eluant and testing the various fractions by TLC. The solvent was evaporated off the middle fractions to give 2.4 g of the 1-[2,4-dichloro-beta-[[p-(phenylthio)benzyl]oxy] phenethyl]imidazole as a yellowish oil, showing a single spot on TLC.
METHOD 2:
0.66 g of sodium hydride (50% in oil) were added at 20-30°C and under nitrogen atmosphere to 3.86 g of 1-(2',4'-dichlorophenyl)-2-(N-imidazolyl) ethanol in 15 ml of dimethylsulphoxide (dried on calcium hydride). The mixture was heated under stirring at 50-60°C until gas emission was over. After cooling to 20-25°C, 0.5 g of potassium iodide were added and slowly a solution of 3.51 g of 1-chloromethyl-4-phenylthiobenzene in 4 ml of dimethylsulphoxide was dropped in. The mixture was stirred at 20-25°C until addition of the 1-chloromethyl-4-phenylthiobenzene was over. The mixture was then poured into 150 ml of water and extracted with diethyl ether. To the etheric solution, after drying on anhydrous sodium sulphate, was added excess 4 N nitric acid solution in diethyl ether: the desired product precipitated as nitrate, an oil which solidified on standing. After standing for 20 hours, the etheric liquid was decanted off and the residue was crystallized from ethanol. The nitrate thus obtained, not completely pure, was dissolved in water and excess sodium carbonate was added in order to liberate the base which was then extracted with ethyl acetate. The base, obtained by filtration, was purified on a silica gel column using ethyl acetate as eluant. The combined fractions containing the desired product were evaporated to dryness. The residue was dissolved in diethyl ether, again transformed into the nitrate and crystallized from ethanol. Yield: 3.1 g of a white crystalline powder, melting at 136°C; λmax 252 nm (methanol).

brand name

Lomexin

Therapeutic Function

Antifungal

Fenticonazole nitrate Preparation Products And Raw materials

Raw materials

Preparation Products

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Fenticonazole nitrate Suppliers

J & K SCIENTIFIC LTD.
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010-82848833 400-666-7788
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86-10-82849933
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jkinfo@jkchemical.com
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China
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1-(800)-881-8210
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615-250-9817
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inquiries@lgmpharma.com
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Shanghai Longsheng chemical Co.,Ltd.
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021-58099652-8005 13585536065
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021-58099609
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Chemsky(shanghai)International Co.,Ltd.
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021-50135380
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Hangzhou Yuhao Chemical Technology Co., Ltd
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+86-571-82880190
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Dalian Meilun Biotech Co., Ltd.
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TOKYO CHEMICAL INDUSTRY CO., LTD.
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03-3668-0520
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View Lastest Price from Fenticonazole nitrate manufacturers

WUHAN FORTUNA CHEMICAL CO., LTD
Product
Fenticonazole nitrate 73151-29-8
Price
US $0.00/Kg/Bag
Min. Order
1KG
Purity
99%-101%; USP/EP
Supply Ability
100KGS
Release date
2021-09-13
Shaanxi Dideu Medichem Co. Ltd
Product
Fenticonazole 73151-29-8
Price
US $0.01-1.00/KG
Min. Order
1KG
Purity
99%
Supply Ability
50 tons
Release date
2020-05-12
Shanxi Naipu Import and Export Co.,Ltd
Product
Fenticonazole nitrate 73151-29-8
Price
US $100.00/KG
Min. Order
1KG
Purity
99
Supply Ability
5tons
Release date
2021-10-21

73151-29-8, Fenticonazole nitrateRelated Search:


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