Molecular Formula | C26H30Cl2F3NO |
Molar Mass | 500.42 |
Density | 1.244±0.06 g/cm3 (20 ºC 760 Torr) |
Water Solubility | 0.59mg/L(37 ºC) |
Storage Condition | 2-8°C |
Physical and Chemical Properties | Halofanide hydrochloride (Halofantrine Hydrochloride):C26H30C12F3NO?HCl. [36167-63-2]. There are two kinds of crystals: melting point 93-96 ℃; melting point 203-204 ℃. Halofanide glycerophosphonate (Halofantrineβ-Glycerophosphate):C29H39C12F3NO7P. [96849-12-6]. White crystal, melting point 60~65 ℃. |
Use | is an old antimalarial drug discovered in the 30's of the 20th century. It is as effective against Plasmodium falciparum as chloroquine and can cure patients infected with a chloroquine-resistant parasite. For malaria. |
production method | condensation of 2, 4-dichloro-6-nitrobenzaldehyde with 4-trifluoromethylphenylacetic acid, compound (I) was obtained. The compound (II) was obtained by re-reducing the nitro group to the amino group. First, the diazotization of nitrous acid is carried out, and then the phenanthrene ring (III) is synthesized by coupling ring under the action of strong acid. This is the classical Pschorr reaction. This is followed by reduction to alcohol and oxidation to aldehyde (V) with lead acetate. Reformatski condensation was carried out with N,N-di-N-butyl bromoacetamide and zinc, and the product was reduced with diborane to obtain Halo-Pan Group. Under stirring, 14.0g of halotoxoid was added to 4.8g of β-glycerophosphonic acid in 50% aqueous solution, followed by addition of 100 of ethanol and heating at about °c. The precipitated white precipitate was collected by filtration to obtain Halo-Pan-group glycerophosphonate. |