alpha-difluoromethylornithinehydrochloridehydrate
Eflornithine Hydrochloride
CAS: 68278-23-9
Molecular Formula: C6H13ClF2N2O2
alpha-difluoromethylornithinehydrochloridehydrate - Names and Identifiers
alpha-difluoromethylornithinehydrochloridehydrate - Physico-chemical Properties
| Molecular Formula | C6H13ClF2N2O2 |
| Molar Mass | 218.63 |
| Melting Point | 181-184°C |
| Boling Point | 347°C at 760 mmHg |
| Flash Point | 163.7°C |
| Water Solubility | H2O: >10 mg/mL, soluble |
| Solubility | H2O: >10mg/mL, soluble |
| Vapor Presure | 9.72E-06mmHg at 25°C |
| Appearance | solid |
| Color | white |
| Use | For female hair removal |
| In vivo study | Eflornithine is the only new molecule registered for the treatment of human African trypanosomiasis over the last 50 years. It is the drug used mainly as a back-up for melarsoprol refractory Trypanosoma brucei gambiense cases. In subjects with excessive, unwanted facial hair, eflornithine 15% cream is superior to placebo in reducing hair growth. After 24 weeks' treatment, 58% of eflornithine and 34% of placebo subjects have at least some improvement in facial hirsutism. The hair growth inhibitory activity of eflornithine is significantly enhanced when the eflornithine cream is applied onto a mouse skin area pretreated with microneedles. Treatment of coarctation hypertensive rats with eflornithine results in a normalization of the contractile intensity to KCI and norepinephrine and relaxations to acetylcholine by 14 days of hypertension. |
alpha-difluoromethylornithinehydrochloridehydrate - Risk and Safety
| WGK Germany | 3 |
alpha-difluoromethylornithinehydrochloridehydrate - Reference Information
| treatment of African trypanosomiasis | The fluoroalfa amino acid, eflornithin, a specific irreversible inhibitor of ornithine decarboxylase, it was approved in 1990 for the treatment of African trypanosomiasis and female facial hair overgrowth. efiuorornithine: This molecule is less toxic than melarsine and was registered in 1990. It is only effective against Trypanosoma brucei. The course of treatment is complex and difficult to administer. In particular, in rural Africa, where the incidence of sleeping sickness is high, the availability of medical equipment and medical personnel has hampered the implementation of such treatment programmes. In 2009, a combination therapy called NECT was developed by international cooperation organizations, including the non-profit drug research and development organization DNDi (neglected diseases drug initiative) and MSF, the combined use of nifuroxime and efluoro-ornithine is simpler than the use of efluoro-ornithine alone, and the safety and therapeutic effect are also greatly improved. It simplifies the use of efloroornithine by reducing the duration of treatment and the number of intravenous infusions, but unfortunately, it has not been studied whether it is effective against Trypanosoma brucei. Nifuroxime is registered for the treatment of American trypanosomiasis, but not for the treatment of human African trypanosomiasis. However, after clinical trials provided safety and efficacy data, the combination of the drug and eflumine has been included in the WHO list of essential medicines, it is currently recommended as a first-line treatment for infection of the Gambia type. World Health Organization (WHO) for this purpose, both drugs and a package containing all the materials required for their use are provided free of charge to the regionally endemic countries. |
| synthesis method | 15THF was cooled to -80 °c and 2.82L of diisopropylamine was added under nitrogen protection, further, 12L of a 15% butyl lithium solution in hexane was added at a rate that maintained the temperature of the reaction solution at -75 to -80 °c. A solution of N,N'-dibenzylidene ornithine methyl ester (I) in 15L of THF was then added. After the addition, the temperature was slowly raised to 35 to 40 ° C., and the reaction was carried out by substituting nitrogen with a bubbling of monochlorodifluoromethane. 20L of saturated sodium chloride solution and 75L of isopropyl ether were added, the organic layer was separated and the aqueous layer was extracted. The extracts and the organic layer were combined, washed with saturated sodium chloride solution, and concentrated to a residual oil, I .e., compound (II). The oil and 30 11 mol/L hydrochloric acid were reacted at room temperature for 3H and hydrolyzed. After completion of the reaction, the reaction mixture was extracted with chloroform, and the extract was discarded. The extracted aqueous layer was diluted with 6L of water, adjusted to pH 3.3, heated, filtered, washed, and recrystallized to give eflumine. |
| biological activity | eflornitine hydrochloride (DFMO hydrochloride) is a specific irreversible inhibitor of the enzyme ornithine decarboxylase. Eflornithine hydrochloride (DFMO hydrochloride) is useful in the study of African trypanosomiasis and facial hair overgrowth in women. |
| Use | for female hair removal |
Last Update：2024-04-09 15:16:52
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