Milbemycin Oxime Antiparasitic Drug Insecticide

English name：Milbemycin oxime

CAS number：129496-10-2

Molecular formula：2C32H45NO7.2C31H43NO7

Molecular weight 2194.78

EINECS number 206-141-6

Related categories: Raw material intermediates-API; medical raw materials; additives; organic raw materials; veterinary drug API; raw materials; microbial metabolites; pharmaceutical intermediates; anti-parasitic drugs; small molecule inhibitors; Inhibitors; small molecule inhibitors, day Chemicalbook ran products; APIsforVeterinary; pharmaceutical raw materials; API; API; pharmaceutical chemical materials; chemical raw materials; pharmaceutical raw materials; anti-parasitic; medical raw materials; reagents; veterinary drug raw materials; chemical intermediates; chemical reagents

melting point：169.6-177.4°

Flash point：412℃

density 1.35±0.1 g/cm3(Predicted)

condition of storage ：Store at -20°C

Solubility DMSO: 100.0 (maximum concentration mg/mL); 91.13 (maximum concentration mM)

Form: a crystalline solid

Color ：white to beige white

Stability: Hygroscopicity

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Overview
Milbesoxime (MilbemycinOxime) is a macrolide antibody and an oxime derivative of milbeemycin A3 and A4.

Application
In 1997, Taiwan launched the pulse heart with milbesoxime as the main ingredient, produced by Taiwan Novartis Company Limited, as the prevention of heartworm and intestinal parasites, which was the first application of milbesoxime in China. Mirbeoxime has a broad spectrum of antiparasitic effects and good effects on in vivo and in vitro parasites, especially nematodes and arthropods.

Side effect
Although milbe oxime side effects are very rare, but because of different animal state, infection state is not the same and dosage, some will appear after medication pet extreme depression, tired Chemicalbook food, drowsiness, salivation, vomiting, diarrhea, epilepsy pain, body deficiency poisoning symptoms, or swelling, urticaria, acute diarrhea, shock, etc., so still need to be under the guidance of veterinary medicine.

Biological activity
Milbemycin Oxime Is a broad-spectrum antiparasitic drug with active effects against worms and mites.

Chemical property
Milbeoxime is an oxime derivative of milbeamycin D, which contains hydroxyl groups in its structure at carbon-5 and carbon-7 positions and separate double bonds at carbon-3 and carbon-14 positions, with carbon-8 and carbon-11 forming a conjugated diene structure. The Sankyo group underwent chemical transformation of the allyl hydroxyl group at position 5, which synthesized a series of oxime derivatives from milbemycin A4 and A3, and the carbon-5 hydroxyl group was oxidized to ketones by Chemicalbook manganese dioxide in a quantitative manner. This ketone-containing α, β -hydroxylamine hydrochloride, reacts in dioxane-methanol-water to produce a series of 5-oxime milbedemins. Milbesoxime mainly contains milbesamycin A3 oxime and A4 oxime, where milbesamycin A4 oxime should not be less than 80% and A3 oxime should not exceed 20%. It is a yellow crystalline powder, with odor, easily soluble in organic solvents such as benzene, acetone, ethanol, methanol and chloroform, but insoluble in water.

Use
Milbeoxime is a specific drug for the control of internal and external arasites in dogs and cats. It can effectively effect the control of hookworm, round worm, whip worm, roundworm and other internal parasites, as well as hair follicle worm, scabies, lice, fleas and other external parasitic Chemicalbook parasites. Mirbeoxime can paralyze the parasite and die, without adverse effects on nerve conduction in mammals, or even on sheepdogs, which are generally considered to have high blood-brain barrier permeability.

Methods of production
(1) Oxidation reaction: with milbeomycin as raw material, hypochlorite or chlorite as oxidant, piperidine nitrogen oxide radical as catalyst, halide as cocatalyst, reaction in dichloromethane solvent at-5~15℃ for 0.5~4h, the reaction product Chemicalbook after treatment to obtain the intermediate milbenone;

(2) Oxime reaction: methanol and 1,4-dioxane as reaction solvent, with hydroxylamine hydrochloride as oximing reagent, reaction at 25~35℃ for 10-16 h, after treatment and purification.

Safety Information
Dangerous Goods Transport No.2588
WGK Germany3
Hazard Grade 6.1 (b)
Packaging category III
H. S code：2932206000
toxicity LD50 orally in mice: 1000-1500 mg/kg (Ciba-Geigy)

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