- Method for using tylosin D as raw material to prepare tilmicosin
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The invention relates to a method for using tylosin D as a raw material to prepare tilmicosin. The method comprises the steps of using tylosin D as the raw material, oxidizing a C[20]position primary dydroxide radical into a formyl group through a selective oxidant to obtain a first midbody, then conducting hydrolysis and decarbonization on mycarose to obtain a second midbody, and making formic acid and 3,5 dimethyl piperidine subjected to a reductive ammonolysis reaction to obtain the product tilmcosin. According to the method for using tylosin D as the raw material to prepare tilmicosin, tylosin D is adopted as the raw material, through the specific selective oxidant, tylosin D is converted into an effective component in compound tilmicosin and is prevented from being converted into impurities, thus a new path is opened up for the preparation of tilmicosin, and the problems that the impurities are high in residual rate and the yield rate is low when tylosin is adopted as an original raw material to prepare tilmicosin are solved.
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Paragraph 0058; 0059; 0060
(2017/07/20)
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- Novel Semisynthetic Oxo and Alkyl Macrolide Antibacterials and Related Derivatives
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An efficient method of protecting the 10,11-double bond in dienone and epoxy enone 16-membered macrolides has been developed.This involves Michael addition of thioacetic S-acid to the 10,11-ene to give exclusively the 11-acetylthio derivatives, which can be smoothly deprotected by treatment with fluoride ion.The protected intermediates have been used to prepare a novel class of macrolide antibacterials in which the aldehyde group has been converted into an alkyl ketone by reaction with the appropriate diazoalkane.Thus 20-oxo analogues of rosaramicin, 12,13-de-epoxy-12,13-dehydro-rosaramicin, tylosin, and desmycosin have been prepared.The reaction of diazomethane with unprotected macrolides has also been studied including the synthesis of 18-C-methyl-3''-O-propionyl-leucomycin A5.Derivatives in which the 20-formyl group has been replaced by metal and by halogeno groups, as well as derivatives having a 2,3-ene are described.A number of base-catalyzed rearrangement products including desmycosin 8β,20α-aldol and desmycosin 8α,20β-aldol are also described.
- Fishman, Andrew G.,Mallams, Alan K.,Puar, Mohindar S.,Rossman, Randall R.,Stephens, Richard L.
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p. 1189 - 1210
(2007/10/02)
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- TOTAL SYNTHESIS OF TYLOSIN
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Tylosin has been synthesized by regio- and stereoselective introduction of the amino disaccharide moiety and D-mycinose onto the previously synthesized 16-membered-ring aglycone.
- Tatsuta, Kuniaki,Amemiya, Yoshiya,Kanemura, Yoshinobu,Takahashi, Hideaki,Kinoshita, Mitsuhiro
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p. 3375 - 3378
(2007/10/02)
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- 3-Imino-1,2,4-benzotriazine-1-oxides
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New 3-Imino-1,2,4-benzotriazine-1-oxides of formula I SPC1 wherein R represents an alkyl, alkenyl or haloalkyl radical, a phenyl or aralkyl radical optionally substituted by alkyl, alkoxy, haloalkyl, halogen or hydroxy, X and Y each independently represent hydrogen, halogen, an alkyl or alkoxy radical, or one of the two symbols represents a phenoxy or phenylsulphonyl radical optionally substituted by halogen, alkyl, haloalkyl and/or alkoxy which are active against harmful microorganisms are disclosed.
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