LUMEFANTRINE

Benflumetol; Coartem; DL-Benflumelol; (1R,S)-2-Dibutylamino- 1-{2,7-dichloro- 9-[(Z)(4-chlorobenzylidene)- 9H-fluoren-4-yl}-ethanol; (+-)-2,7-Dichloro-9-((Z)-p-chlorobenzylidene)- alpha ((dibutylamino)methyl) fluorene-4-methanol; (Z)-2,7-Dichloro-9-((4-chlorophenyl)methylene)- alpha((dibutylamino) methyl)- 9H-fluorene-4-methanol; 2-(Dibutylamino)-1-[(9Z)-2,7-dichloro-9-[(4- chlorophenyl) methylidene]fluoren-4-yl]ethanol;

 LUMEFANTRINE

 

PRODUCT IDENTIFICATION

CAS RN

82186-77-4

EINECS RN

 

FORMULA

C30H32Cl3NO

MOLE WEIGHT

528.94

 

PHYSICAL AND CHEMICAL PROPERTIES

PHYSICAL STATE

yellowish crystalline powder

MELTING POINT

125 - 130 C

BOILING POINT

 

DENSITY

1.252

SOLUBILITY IN WATER

Insoluble (soluble in chloroform and in most organic solvents, slightly soluble in propanol, almost insoluble in ethanol)

pH

 

VAPOR DENSITY

 

REFRACTIVE INDEX

 

FLASH POINT

 

 

STABILITY AND REACTIVITY
STABILITY Stable under normal conditions

INCOMPATIBLE MATERIALS

Strong oxidizing agents.

DECOMPOSITION PRODUCTS

Carbon oxides. nitrogen oxides

POLYMERIZATION Has not been reported

NFPA RATINGS

Health: 2, Flammability: 0, Reactivity: 0

 

SAFETY

HAZARD NOTES

 

EYE

 

SKIN

 

INGESTION

 

INHALATION

 

CHRONIC

 

 

TRANSPORT & REGULATORY INFORMATION

UN NO.

 
HAZARD CLASS

 

PACKING GROUP

 

HAZARD SYMBOL

 

RISK PHRASES

 

SAFETY PHRASES

 

 

EXTERNAL LINKS & GENERAL INFORMATION

Artemether and lumefantrine combination is a fixed dose artemisinin-based combination therapy (ACT) combining artemether, an artemisinin derivative, and lumefantrine, a synthetic antimalarial drug. Chemical formula of artemether is (3R,5aS,6R,8aS,9R,10S,12R,12aR)-Decahydro- 10-methoxy-3,6,9-trimethyl- 3,12-epoxy-12H-pyrano[4,3-j]-1,2-benzodioxepin whereas chemical formula of lumefantrine is (1R,S)-2-Dibutylamino- 1-{2,7-dichloro- 9-[(Z)(4-chlorobenzylidene)-9H-fluoren-4-yl}-ethanol. Artemether is a sesquiterpene lactone derived from artemisinin. Artemisinin is a compound derived from the sweet wormwood plant and has been used for centuries in traditional Chinese medicine to treat fever. Lumefantrine is a synthetic aryl-amino alcohol antimalarial (quinine, mefloquine and halofantrine are members of the same group). (http://www.malaria-ipca.com/)

Of these four latest kinds of antimalarial drugs, two of them, artemisinin derivatives and pyronaridine, were drawn from the Chinese pharmacopoeia. A third Chinese type of drug, lumefantrine, has recently been identified as a promising candidate for use in therapy. Lumefantrine (also called benflumetol, code no. CGP 56695; 1:1 racemate of the dextrogyre and levogyre enantiomers) is a fluorene derivative (2,3-benzindene) that belongs to the aminoalcohol class. The compound was synthesized at the Academy of Military Medical Sciences, Beijing, China, and has undergone preliminary clinical studies in China. Lumefantrine, in combination with artemether (called coartemether), was registered for the oral treatment of malaria in China in 1987. In early clinical studies conducted in China, cure rates of 96% (n = 314 patients) and 92.5% (n = 40 patients) were reported with oral lumefantrine alone (a total dose of 2,000 mg in divided doses over 4 days) and lumefantrine-artemether oral combination (1,920 mg of lumefantrine-320 mg of artemether in divided doses over 3 days), respectively. The clinical efficacy of the lumefantrine-artemether combination has been confirmed recently in China, Thailand, and The Gambia. (http://aac.asm.org/)

 

SALES SPECIFICATION

APPEARANCE

yellowish crystalline powder

IDENTIFICATION

pas teat A,B

ASSAY

99.0% min

LOSS ON DRYING

0.5% max

RELATED COMPOUNDS

1.0% max

HEAVY METALS,

10ppm max

RESIDUE ON IGNITION

0.1% max

MELTING POINT

125 - 130 C

 

PRICE

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