- Preparation method of dacotinib
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The present invention discloses a method of preparation of dacotinib, comprising the following steps: (N- (3-chloro-4-fluorophenyl) -7-fluoro-6-nitro-4-quinazoline) in a base / methanol system to undergo a methyl oxidation reaction, to compound 02 (N- (3-
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Paragraph 0051-0064
(2022/01/10)
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- Preparation method of lung cancer targeted drug Dacomitinib
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The invention provides a preparation method of a lung cancer targeted drug Dacomitinib. Specifically, 3-amino-4-methoxybenzonitrile is used as a raw material and is subjected to a condensation reaction with 4-(piperidine-1-yl) butyl-2-enoyl chloride to obtain a formula III, a compound shown in the formula III is nitrified to obtain a formula IV, the formula IV is subjected to a cyano hydrolysis reaction to obtain a formula V, the formula V is subjected to a reduction reaction to obtain a formula VI, the formula VI is subjected to a condensation cyclization to obtain a formula VII, the formula VII is subjected to a chlorination reaction to obtain a formula VIII, and the formula VIII is subjected to a coupling reaction to obtain the final product Dacomitinib. The preparation method disclosed by the invention is simple, mild in reaction condition, high in safety, low in raw material cost, relatively high in reaction yield and suitable for industrial large-scale production.
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- Preparation method of Dacomitinib
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The invention provides a preparation method of Dacomitinib. Specifically, 3-amino-4-methoxybenzonitrile is used as a raw material and is subjected to a condensation reaction with 4-(piperidine-1-yl) butyl-2-enoyl chloride, a product is subjected to nitration and reduction, condensation with DMF-DMA is performed, and cyclization reaction with 3-chloro-4-fluorophenylamine is performed to prepare the Dacomitinib. The preparation method has the advantages of simple and safe synthesis route and operation, easily available raw materials, simple post-treatment and high yield, and is suitable for industrial production.
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- Preparation method of dacrotinib
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The invention provides a preparation method of dacrotinib. Specifically, methyl 3-amino-4-methylbenzoate used as a raw material is subjected to condensation, nitration, reduction, ring closing, halogenation and coupling to obtain the dacotinib. The preparation method provided by the invention has the advantages of cheap and easily available raw materials, simple reaction and post-treatment operation and high yield, and is suitable for industrial production.
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- Preparation method of dacomitinib intermediate
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The invention provides a preparation method of a dacomitinib intermediate. The preparation method comprises steps shown in the specification. The invention provides the novel preparation method of the dacomitinib key intermediate, the intermediate is short in synthetic route, mild in reaction condition, short in reaction time and simple in separation and purification method, raw materials and reagents are conventional reagents, the cost is low, the yield of the prepared product is high, and the method is very beneficial to industrial production and popularization and has a good application prospect.
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- Preparation method of dcotinib
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The invention discloses a preparation method of Dacomitinib. The preparation method comprises the following steps: methyl oxidation, reduction and condensation reaction. The preparation method disclosed by the invention is simple and effective in process, simple and reliable to operate, high in economic benefit and more suitable for industrial production; the prepared Dacomitinib is high in purity and high in overall yield.
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- Preparation method of Dactinib key intermediate
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The invention provides a preparation method of a Dacomitinib key intermediate. The preparation method comprises the following steps: taking Dacomitinib as a raw material; the intermediate is short in synthetic route, mild in reaction condition, short in reaction time, simple in separation and purification method and low in cost, raw materials and reagents are all conventional reagents, and the prepared product is high in yield and quite beneficial to industrial production and popularization and has good application prospects.
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- Highly-efficient preparation method for lung cancer targeting drug
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The invention discloses a highly-efficient preparation method for a lung cancer targeting drug. The highly-efficient preparation method comprises the following steps: with N'-(2-cyano-5-methoxy-4-nitrophenyl)-N,N-dimethylformamide (II) as an initial raw material, subjecting the N'-(2-cyano-5-methoxy-4-nitrophenyl)-N,N-dimethylformamide (II) to hydrogenation reduction, pressure-reduced concentration, acid-addition salification, alkaline-addition desalification, an acylation reaction and a Dimroth rearrangement reaction in sequence so as to obtain dacomitinib (VI), and allowing the dacomitinib to react in a 2-methyltetrahydrofuran aqueous solution so as to obtain dacomitinib monohydrate (I). According to the invention, by adoption of an acid-addition salification process in the production process, the defects and disadvantages of easy degradation, a large amount of side reaction impurities, low product purity and the like for raw materials in the reaction process in the prior art are overcome.
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- 4-Phenylamino-quinazolin-6-yl-amides
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This invention provides quinazoline compounds of the formula: wherein: R1 is halo; R2 is H or halo; R3 is a) C1-C3 alkyl, optionally substituted by halo; or b) —(CH2)n-morpholino, —(CH2)n-piperidine, —(CH2)n-piperazine, —(CH2)n—-piperazine-N(C1-C3 alkyl), —(CH2)n-pyrrolidine, or —(CH2)n-imidazole; n is 1 to 4; R4 is —(CH2)m-Het; Het is morpholine, piperidine, piperazine, piperazine-N(C1-C3 alkyl), imidazole, pyrrolidine, azepane, 3,4-dihydro-2H-pyridine, or 3,6-dihydro-2H-pyridine, each optionally substituted by alkyl, halo, OH, NH2, NH(C1-C3 alkyl) or N (C1-C3 alkyl)2; m is 1-3; and X is O, S or NH; or a pharmaceutically acceptable salt thereof, as well as processes and intermediate compounds for making them, useful pharmaceutical compositions and methods of using the compounds in the treatment of proliferative diseases.
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Page/Page column 18-20
(2010/02/14)
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