- Preparation method of antitumor drug AZD9291
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The invention relates to a preparation method of an antitumor drug AZD9291. The preparation method comprises the following steps: taking 2-bromo-4-anisidine as a starting raw material; carrying out nitration reaction, grignard reaction, acylation reaction, reduction reaction, grignard reaction and elimination reaction to obtain AZD9291 free alkali. The preparation method disclosed by the inventionhas the beneficial effects of wide source of raw materials, low cost, simple operation, recyclable application of a solvent, low discharge amount of waste liquid, high recovery rate of a product andthe like, and easily realizes industralization.
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Paragraph 0030
(2018/07/30)
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- Osimertinib preparation method
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The present invention relates to an osimertinib preparation method, which comprises: (1) carrying out a nucleophilic substitution reaction on 3-(2-chloro-4-pyrimidinyl)-1-methyl-1H-indole and 4-fluoro-2-methoxy-5-nitroaniline to prepare a compound 1; (2) carrying out a substitution reaction on the compound 1 and N,N,N-trimethylethylenediamine in the presence of an organic alkali to prepare a compound 2; (3) reducing the compound 2 in the presence of a reducing agent to prepare a compound 3; (4) carrying out condensation on the compound 3 and 3-chloropropionyl chloride in the presence of an alkali to obtain a compound 4; (5) carrying out a heat elimination reaction on the compound 4 through heating in the presence of an alkali to prepare a compound 5; and (6) carrying out salification on the compound 5 and methanesulfonic acid under a heating condition to obtain osimertinib. According to the present invention, the osimertinib synthesis process has characteristics of stability, controllability, no high-toxicity solvent is used, energy saving and environmental protection.
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- Preparation method for osimertinib
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The invention provides a preparation method for osimertinib. According to the invention, the raw material 3-chloropropionic acid has low toxicity and stable properties and is easily available; reaction conditions are mild; operation is simple; high-yield high-purity osimertinib can be prepared; and the method is suitable for industrial production.
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Paragraph 0028; 0029; 0033; 0034; 0038; 0039; 0043; 0044
(2018/01/17)
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- Dimethyl sulfonate of compound A, crystal form of dimethyl sulfonate, and medicinal composition containing dimethyl sulfonate
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The invention provides dimethyl sulfonate of a compound A, a crystal form of the dimethyl sulfonate, application of the dimethyl sulfonate of the compound A in preparation of a medicine for preventing and/or treating mammal diseases, and a medicinal composition containing the dimethyl sulfonate of the compound A, wherein the mammals comprise human beings, and the diseases comprise various cancers, preferably non-small cell lung cancer, particularly mutated non-small cell lung cancer.
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Paragraph 0072
(2017/08/28)
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- 2 - (2, 4, 5 - SUBSTITUTED -ANILINO) PYRIMIDINE DERIVATIVES AS EGFR MODULATORS USEFUL FOR TREATING CANCER
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The present invention relates to certain 2-(2,4,5-substituted-anilino) pyrimidine compounds and pharmaceutically acceptable salts thereof which may be useful in the treatment or prevention of a disease or medical condition mediated through certain mutated forms of epidermal growth factor receptor (for example the L858R activating mutant, the Exonl9 deletion activating mutant and the T790M resistance mutant). Such compounds and salts thereof may be useful in the treatment or prevention of a number of different cancers. The invention also relates to pharmaceutical compositions comprising said compounds and salts thereof, especially useful polymorphic forms of these compounds and salts, intermediates useful in the manufacture of said compounds and to methods of treatment of diseases mediated by various different forms of EGFR using said compounds and salts thereof.
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