- THAILANSTATIN ANALOGS
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The invention provides novel cytotoxic compounds and cytotoxic conjugates comprising these cytotoxic compounds and cell-binding agents. More specifically, this invention relates to novel thailanstatin A analogs, useful as cytotoxic small molecule toxins i
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Paragraph 0373; 0376
(2019/04/05)
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- Chemical synthesis method of 3-isoxazolyl benzyl acetate
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The invention discloses a chemical synthesis method of 3-isoxazolyl benzyl acetate. The chemical synthesis method comprises the following steps: S1, carrying out addition reaction through butene nitrile and bromine gas and generating 3-amino-5-methylisoxazole in the presence of a hydroxylamine derivative; S2, preparing 3-amino-5-methylisoxazole into diazonium salt under low temperature under the action of catalysis, carrying out substitution reaction on the diazonium salt in a hydrochloric acid environment, substituting amino and preparing 3,5-dimethylisooxazole, carrying out demethylation andpreparing 3-chloromethylisoxazole; and S3, adding 3-chloromethylisoxazole and cuprous cyanide into an organic solvent which is dimethyl sulfoxide, reacting and preparing 3-isooxazole acetonitrile. According to the chemical synthesis method of 3-isoxazolyl benzyl acetate, the raw materials are products obtained by directly cracking petroleum; production is carried out by five steps of addition, catalysis, substitution, hydrolysis and esterification; the reaction is rapid; when 3-chloromethylisoxazole as an intermediate is prepared, the yield reaches up to 75%; the production yield is ensured.
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Paragraph 0014-0015; 0018-0019
(2019/02/04)
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- A 3 - isoxazole acetate acid animal pen fat chemical synthesis method
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The invention relates to a chemical synthesis method of 3-isoxazolyl benzyl acetate. According to the invention, chloroacetyl chloride and acetylene are taken as raw materials, the yield of the reaction is increased by addition, condensation, substitution, hydrolysis and esterification steps and an efficient synthesis method is provided for the synthesis of the compound. The synthesis method mainly comprises steps of adding acetylene, chloroacetyl chloride, catalyst aluminum chloride and a solvent tetrahydrofuran into the reaction vessel, reacting, and separating to obtain 1,4-dichloro-3-butenone after the reaction is completed; adding 1,4-dichloro-3-butenone and ammonium sulfate into a methanol or ethanol solvent, controlling the reaction temperature, and reacting to obtain 3-chloromethyl isoxazole; preparing 3-isoxazole acetonitrile; adding 3-isoxazole oxazol-acetonitrile into hydrochloric acid for hydrolyzing to obtain 3-isoxazole acetic acid; adding 3-isoxazole acetic acid and benzyl alcohol into a dichloromethane or trichloromethane solvent, and adding thionyl chloride and a catalyst N, N-dimethyl-formamide for reacting to obtain 3-isoxazolyl benzyl acetate.
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Paragraph 0027; 0038; 0043; 0048; 0049
(2018/04/01)
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