217500-96-4Relevant articles and documents
Preparation method of tulathromycin
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Paragraph 0022-0033, (2021/05/05)
The invention relates to a synthetic method of tulathromycin. Under the action of illumination and a specific catalytic system, rapid, efficient and pollution-free synthesis of tulathromycin is realized. Compared with the existing synthetic method, the synthetic method provided by the invention is simple to operate, mild in condition and capable of meeting the requirement of large-scale industrial production.
Synthesis of terramycin
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Paragraph 0020-0021, (2022/01/08)
The present invention relates to the synthesis of terramycin, specifically (2R,3S,4R,5R,8R,10R,11R,12S,13S,14R)-2-ethyl-3,4,10-trihydroxy-13-[[3S,4S,6R,8R]-8-methoxy-4,8-dimethyl-1,5-dioxa snail [2,5]octyl-6-yl]oxo) 3,5,8,10,12,14-hexamethyl-11-[3,4, 6-Tr
Preparation method for tulathromycin
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Paragraph 0200; 0210-0212; 0213; 0223-0225; 0265; 0275-0277, (2020/07/02)
The invention provides a preparation method for tulathromycin, and belongs to the technical field of drug synthesis. The method comprises the following steps: mainly by using dihydroerythromycin (9-deoxo-9a-aza-9a-homoerythromycin A) as a raw material, performing a hydroxyl protection reaction, performing a selective oxidation reaction of 4'-hydroxyl to generate a ketone, performing an epoxidationreaction to generate an epoxide, performing deprotection, and performing a ring-opening reaction to introduce n-propylamine to generate the target product tulathromycin. In the method, an oxidizing agent for the selective oxidation reaction of the 4'-hydroxyl is hydrogen peroxide or a Dess-Martin periodinane, so that the method avoids the use of equivalent or excessive amounts of a high-valent metal oxidizing agent, has low costs and mild reaction conditions, and improves the yield and purity of the product.
Method for synthesizing oxytetracycline and oxytetracycline phosphate (by machine translation)
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, (2020/04/22)
Step A product shown in Formula is obtained by dissolving, a product of: Formula I with a product shown by subjecting a product shown II in Formula to a reaction; to obtain a product having a hydroxyl: protection product II as shown in Formula I, and a ca
Preparation method of tulathromycin
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Paragraph 0058-0060, (2020/04/02)
The invention provides a preparation method of tulathromycin, and belongs to the field of pharmaceutical chemicals. The method comprises the following steps of: reacting azithromycin serving as a rawmaterial with phenyl chloroformate to protect hydroxyl to obtain protected nitrogen azithromycin, oxidizing the hydroxyl into a ketone group by oxidation, epoxidizing, deprotecting, and reacting withn-propylamine to obtain tulathromycin. The product produced by the method has the characteristics of high purity, high yield, low cost, simple operation and stable process.
METHOD AND INTERMEDIATE FOR PREPARING TULATHROMYCIN
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, (2019/02/05)
A method and an intermediate for preparing a tulathromycin. The method includes the following step: in an organic solvent, subjecting a compound represented by formula (II) and an n-propylamine to a ring-opening addition shown below to obtain a tulathromycin represented by formula (I), wherein the organic solvent is a 1,2-propandiol. Tulathromycin obtained using the method has a high purity, with an HPLC purity being 95% and above, and up to 99% and above, satisfying a required purity for preparing a tulathromycin as a pharmaceutical formulation. The method has a high yield, is simple to operate, and is more suitable for industrial production.
Method for preparing tulathromycin
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, (2018/05/30)
The invention relates to a novel method for preparing tulathromycin. The method includes the steps that 3,4-acetonylidene protected demethylazithromycin is used as a starting material, a 2-hydroxyl group is firstly protected, then a 4-hydroxyl group is oxidized to a carbonyl group under Swern conditions, TMSCN is used for performing a cyano group addition reaction on the carbonyl group under the action of TBAF, a resulting intermediate compound is subjected to a hydrogenation reaction in the presence of HOAc with Pd/C as a catalyst, the cyano group in the compound is converted into an amine methyl group while a 2-hydroxy group protecting group and 3,4-acetonylidene protection are removed, and finally under the action of base, an amine methyl compound is reacted with 1-halogenated propane to achieve the preparation of tulathromycin.
Tulathromycin oxalate
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, (2017/12/27)
The invention discloses salt of tulathromycin, particularly oxalate, a preparation method of tulathromycin oxalate and application of tulathromycin oxalate to preparation of tulathromycin.
Salt for tulathromycin intermediate
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, (2018/01/11)
The invention discloses a salt for preparing a tulathromycin intermediate, and particularly relates to oxalate and a preparation method thereof as well as application of the oxalate in a method for preparing tulathromycin.
A synthetic Alterra cephalosporin new route
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Paragraph 0072-0074, (2017/11/16)
The invention discloses a new route for synthesizing tulathromycin. The new route for synthesizing the tulathromycin is different from the previous epoxidation reaction, ring-opening reaction and the like reaction process. The new route for synthesizing the tulathromycin uses Passerini reaction, all the groups are led in by one time, and then the tulathromycin is obtained through Clemmensen reaction and hydrogenation reduction reaction. The new route for synthesizing the tulathromycin includes steps that taking hydroxyl protecting demethylation azithromycin, generating hydroxyl protecting ketone (compound I) through oxidation reaction, leading amido bond and cyclopropyl to a ketone-hydroxyl group position, generating (compound II), reducing the hydroxyl into methylene through Clemmensen reaction, generating (compound III), carrying out hydrogenation and ring opening on cyclopropyl to generate n-propyl through ring-opening reaction, and obtaining the tulathromycin (compound IV). The new route for synthesizing the tulathromycin is simple in process, easy to implement, easy to obtain reaction reagent, moderate in reaction condition, high in selectivity, less in by-product, easy to purify and low in facility request.
