Raw material intermediates Milbemycin Oxime Powder

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Milbemycin Oxime Powder Usage and Synthesis.

In 1997, the first application of Milbemycin in China was the introduction of Milbemycin, with Milbemycin oxime as the main ingredient, as an internal drug for the prevention of heartworm and intestinal parasites in dogs and cats by Novartis Corporation of Taiwan. Milbemycin has a broad-spectrum antiparasitic effect, with good anthelmintic effect on internal and external parasites, especially nematodes and arthropods.

Uses of Milbemycin Oxime.

Milbemycin is currently the most effective drug for the control of internal and external parasites in dogs and cats, which can effectively control heartworm, efficiently control internal parasites such as hookworms, roundworms, whipworms, roundworms, ascarids and other internal parasites, as well as external parasites such as hairy bursa, mange, lice, fleas and other external parasites.

Milbemycin can paralyse and paralyse the parasites to death, and will not adversely affect nerve conduction in mammals, and will not even have an effect on sheepdogs, which are generally considered to have a high permeability of the blood-brain barrier.

Characteristic of Milbemycin Oxime.

Milbemycin oxime is an oxime derivative of milbemycin D. The structure of milbemycin D contains hydroxyl groups at the carbon-5 and carbon-7 positions, separate double bonds at the carbon-3 and carbon-14 positions, and carbon-8 and carbon-11 forming a conjugated diene structure.

Chemical conversion of the allyl hydroxyl group at position 5 by the Sankyo group led to the synthesis of a series of oxime derivatives from milbemycin A4 and A3, where the carbon-5 hydroxyl group was oxidised in a stoichiometric manner by manganese dioxide to a ketone.

This ketone-containing α,β-hydroxylamine hydrochloride reacts in dioxane-methanol-water to produce a series of 5-oxime milbemycins. Milbemycin oxime mainly contains milbemycin A3 oxime and A4 oxime, of which milbemycin A4 oxime should not be less than 80% and A3 oxime should not be more than 20%.

It is yellow crystalline powder with odour, easily soluble in organic solvents such as benzene, acetone, ethanol, methanol and chloroform, but insoluble in water.

Production Method of Bulk Milbemycin Oxime Powder.

(1) Oxidation reaction: using milbemycin as raw material, hypochlorite or chlorite as oxidising agent, piperidine nitrogen-oxygen radicals as catalysts, halides as co-catalysts, reacting in dichloromethane solvent at -5~15°C for 0.5~4h, the reaction products were post-treated to obtain intermediate products of milbemycin;

(2) Oximisation reaction: methanol and 1,4-dioxane were used as reaction solvents, hydroxylamine hydrochloride was used as oximisation reagent, and the reaction was carried out at 25~35°C for 10~16h, and milbemycin oxime was obtained after post-treatment and purification.

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