- Preparation method of mecitinib raw material (by machine translation)
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The method comprises the following steps: preparing,methyl 3 -(-ethyl-)-amido phenol, dichloro - 5 5-methoxyaniline (by reaction with potassium chloride) sodium 2,4 - to generate (dichloro - 5 5-methan)-methaneth, 2,4 -amidobenzylether (in a chlorine substitution reaction). 2,4 - The method comprises the following steps: reacting m-methyl-methanethinonylphenol and hydrogen peroxide, to generate, dichloro - 5 5-methoxyaniline. The method comprises the following steps of reacting m-aminophenol as a raw material to synthesize methyl chloride 2,4 - potassium, and benzoyl (and reacting; with chloromethane in, a mixture) of, sodium, chloride and methyl chloride, and reacting with chloromethane in a reaction condition. (by machine translation)
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Paragraph 0031; 0034; 0037; 0039; 0047; 0049
(2020/05/30)
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- A PROCESS FOR THE PREPARATION OF BOSUTINIB
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The present invention provides an improved process for the preparation of bosutinib and its intermediate 2-cyano-N-(2, 4-dichloro-5-methoxyphenyl)acetamide.
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- New Synthetic Process for Bosutinib
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A new and improved synthetic route to bosutinib is described on a hectogram scale. The key step is the intramolecular cyclization of a 3-(2-aminophenyl)-3-oxopropanenitrile with N,N-dimethylformamide dimethyl acetal to form the 3-cyano-4-hydroxyquinoline ring of 7-(3-chloropropoxy)-6-methoxy-4-oxo-1,4-dihydroquinoline-3-carbonitrile. A practical synthetic method to 2,4-dichloro-5-methoxyaniline is also established. Bosutinib is obtained in 18.0% yield over nine steps from acetovanillone with 98.9% purity (HPLC).
- Mao, Yongjun,Zhu, Chunping,Kong, Ziyang,Wang, Jiao,Zhu, Guoqing,Ren, Xinfeng
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p. 3133 - 3138
(2015/10/19)
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- Herbicidal 1-aryl-4-substituted-1,4-dihydro-5H-tetrazol-5-ones and sulfur analogs thereof
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Herbicidal aryltetrazolinones and thiones of the formula STR1 in which W is oxygen or sulfur; R is alkyl, fluoroalkyl, alkenyl, haloalkenyl, cyanoalkyl, alkylthioalkyl, haloalkoxyalkyl, trifluoromethylthio or alkoxyalkyl; one of X1 and X2 is fluorine, chlorine, or bromine and the other is fluorine, chlorine, bromine, alkyl, nitro or haloalkyl; and Z is a group selected from a variety of substituents including 2-propynyloxy as disclosed and exemplified.
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