- Preparation method of anticancer drug
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The invention relates to a preparation method of an anticancer drug. The anticancer drug is Crenolanib. The preparation method comprises the following steps: taking 2-chlo-8-hydroxyquinoline as a rawmaterial, reacting with trifluoromethanesulfonyl chloride, condensing, dehydrating, performing dehydrochlorination, and performing deprotection to obtain the anticancer drug. Compared with an existingCrenolanib production technology, the preparation method has the characteristics that processes are simple and easy, the purity is high, the yield is high, the processes are short, materials are easyto obtain and low in price, the cost is low, the operation is safe and the like; the industrial production can be conveniently carried out; and technical foundation is supplied for massive productionof the drug and structure-like drugs.
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- Preparation method of drug for treating leukemia
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The invention relates to a preparation method of a drug for treating leukemia. The preparation method comprises 1, preparation of 2-chloro-8-trifluoromethylsulfonyl quinoline, 2, preparation of 2-chloro-8-(piperidin-4-yl)quinolin-carbamic acid tert-butyl ester, 3, preparation of 5-(3-methyl-oxetan-3-methoxy)benzimidazole, 4, preparation of (1-{2-[5-(3-methyl-oxetan-3-yl-methoxy)-benzimidazole-1-yl]-quinolin-8-yl}-piperidin-4-yl-carbamic acid tert-butyl ester, and 5, preparation of (1-{2-[5-(3-methyl-oxetan-3-yl-methoxy)-benzimidazole-1-yl]-quinolin-8-yl}-4-aminopiperidine.
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- Synthesis method of drug for treating leukemia
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The invention relates to a synthesis method of a drug for treating leukemia. The synthesis method comprises that 1, a compound 3-methyl-3-oxetanemethanol and sodium metal undergo a reaction to produce 3-sodium methoxide-3-methyl-3-oxetane, 2, 4-amino-3-nitrochlorobenzene is added into the product obtained by the step 1 so that reddish-orange solids (A1) are obtained, a compound 8-benzyloxyquinolin-2-chlorine and A1 undergo a reaction to produce orange solids A2, 3, the compounds A2, 13g of palladium/carbon and formic acid undergo a reaction, formamidine acetate is added into the reaction product, and the mixture is subjected to reflux and drying so that white-like (or yellow) solids A3 are obtained, and 4, the compounds A3 and benzenesulfonyl chloride undergo a reaction, the product is dried to form maize-yellow solids A4, BINAP, A4, tert-butyl piperidin-4-yl-carbamate and potassium carbonate undergo a reaction, the reaction product is dried to form A5, and the A5 is refined through the step 5 so that a pure product is obtained. In the steps 1 and 2, a one-pot method is used.
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Paragraph 0017
(2018/03/01)
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- PROCESSES FOR THE PREPARATION OF 1-[(BENZOIMIDAZOLE-1YL) QUINOLIN-8-YL] PIPERIDIN-4-YLAMINE DERIVATIVES
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The present invention relates to a process for preparing a compound of the formula (I) or a pharmaceutically acceptable salt, prodrug, hydrate or solvate thereof, wherein R', R2, R3 and R4 are as defined herein. The compound of formula (I) is useful in the treatment of abnormal cell growth, such as cancer, in mammals.
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