- Method for preparing moxidectin
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The invention discloses a method for preparing moxidectin. The method sequentially comprises the following steps: with nemadectin is used as a raw material performing substitution, oxidization and de-protection reactions on allyl chlorocarbonate; The invention discloses a novel synthesis route, wherein used raw materials have characteristics of wide and sufficient source; the method has advantagesof proper cost, simple process, mild reaction conditions of each step, conventional operation, and production cost reducing.
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Paragraph 0046; 0053-0054; 0073-0078
(2020/09/08)
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- A method of chemical synthesis mosictin
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The invention relates to a method of chemically synthesizing moxidectin and belongs to the field of medicinal chemistry. The method comprises the following step: carrying out a reaction on nemadectin as a raw material and 4-chlorophenoxyacetyl chloride as an upper protective agent, and preparing moxidectin through a reaction of four steps: upper protection, oxidization, oximation and deprotection, wherein the reaction sequence of oximation and deprotection can be interchanged without affecting the final reaction product. In the reaction process, the products in upper protection, oxidization and oximation can be recrystallized and extracted through methanol and the like, so that the requirements on the purity of the raw material is reduced, the operating flow is simplified and the reaction cost is lowered.
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Paragraph 0018; 0049; 0050
(2016/12/12)
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- A method of preparing mosictin
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The invention relates to a method for preparation of moxidectin. The method includes subjecting Nemadectin to protective reaction, oxidation reaction, oximation reaction and deprotection reaction in order, thus obtaining moxidectin. Specifically, the protective agent employed in the protective reaction is tert-butyl dimethylchlorosilane, and after the oximation reaction, the solid form crude product obtained by the oximation reaction is subjected to crystallization, and then the deprotection reaction is carried out on the obtained crystal. The method provided by the invention increases the product content, further reduces the difficulty for follow-up utilization of macroporous resin for purification, and improves the column loading amount, reduces the number of column chromatography, maintains or even improves the purity of the final product, and lowers the production cost.
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Paragraph 0101-0104
(2017/03/23)
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- CHEMICAL TRANSFORMATIONS OF S541 FACTORS (A)-(D): PREPARATION AND REACTIONS OF THE 23-KETONES
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The stereoselectivities observed for the reactions of the ketones (5) and (7) with sodium borohydride, Grignard reagents and methoxylamine are described and X-ray data for the oxime (9) are presented.
- Beddall, Nicola E.,Howes, Peter D.,Ramsay, Michael V. J.,Roberts, Stanley M.,Slawin, Alexandra M. Z.,et al.
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p. 2595 - 2598
(2007/10/02)
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