- New Selamectin Intermediates, Preparation Method Thereof And Preparation Method For Selamectin Using The Same
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The present invention relates to a novel intermediate of selamectin which is an antiparasitic drug, a manufacturing method thereof, and an improved method for manufacturing selamectin using the same. More particularly, the present invention relates to: the novel intermediate produced by a four-step synthesis process of a deglycosylation reaction, a hydrogenation reaction, an oxidation reaction, and an oximation reaction; and the improved method of selamectin using the same. The novel intermediate of selamectin according to the present invention has thermal and chemical stability and by using the novel method for manufacturing selamectin of the present invention, it is possible to manufacture selamectin having a higher synthesis yield and purity compared to existing technology.COPYRIGHT KIPO 2019
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Paragraph 0058; 0097-0100
(2019/07/05)
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- Preparation method of high-purity celecampin
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The invention provides an improved selamectin preparation process. The process comprises the following steps: (1) performing hydrogen reduction on doramectin DL in the presence of a Wilson catalyst to obtain an intermediate SL1; (2) recrystallizing and purifying the intermediate SL1 obtained in the step (1) by use of methyl alcohol; (3) desugarizing the intermediate SL1 obtained in the step (2) by use of sulfuric acid to obtain an intermediate SL2; (4) oxidizing the intermediate SL2 obtained in the step (3) by use of manganese dioxide to obtain an intermediate SL3; (5) performing oximation on the intermediate SL3 obtained in the step (4) by use of hydroxylamine hydrochloride to obtain selamectin SL; (6) recrystallizing the crude product SL obtained in the step (5) for three times by use of methylbenzene, acetone and methyl alcohol to obtain purified SL.
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Paragraph 0057-0065; 0066; 0076-0096; 0097; 0102-0109
(2019/07/25)
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- Preparation method of selamectin
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The invention provides an improved preparation technology of selamectin. The improved preparation technology comprises the following steps of (1) in the presence of a Wilson catalyst, reducing the selamectin DL by hydrogen, so as to obtain an intermediate SL1; (2) desugaring the intermediate SL1 obtained in step (1) by an organic solvent hydrochloric acid solution (by dissolving hydrochloric acid gas into an organic solvent), so as to obtain an intermediate SL2; (3) oxidizing the intermediate SL2 obtained in step (2) by manganese dioxide, so as to obtain an intermediate SL3; (4) oximating the intermediate SL3 obtained in step (3) by hydroxylamine hydrochloride, so as to obtain selamectin SL; (5) recrystallizing the crude product of selamectin SL obtained in step (4) by methylbenzene, acetone and methanol, so as to obtain the purified selamectin SL.
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Paragraph 0053; 0054; 0055; 0072; 0073; 0074
(2017/09/18)
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- NEW SYNTHESIS PROCESS OF ANTIPARASITIC DRUG SELAMECTIN
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Provided in the present invention are novel key intermediates of selamectin and the preparation method thereof. Also provided is a new synthesis process, using doramectin as a starting material, and obtaining selamectin via hydrogenation, oxidation, oximation and desugaring. The new process of the present invention has few steps, and is simple to operate, high in yield, low in cost and causes little pollution, and is more suitable for large scale industrial production.
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Paragraph 0041
(2015/02/25)
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