1032903-50-6Relevant articles and documents
Novel sulfinyl anilino pyrimidine derivative and application thereof in preparation of antitumor drugs
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Paragraph 0035; 0046-0048, (2021/10/16)
The invention relates to the field of medicines. A novel sulfinyl anilino pyrimidine derivative is disclosed, and the structural formula of the novel sulfinyl anilino pyrimidine derivative is as shown in the specification. Compared with an existing L858R/T790M inhibitor and EGFR / ALK double-target-target reference substance, the aniline-based pyrimidine derivative containing the sulfoxide group has better antitumor H 1975 activity compared with ALK the prior art BaF3 inhibitor and the EGFR/ALK double ALK-target reference substance. As proved by human liver microsomal experiments, the aniline-based pyrimidine derivatives containing the sulfoxide group in the invention are compared with the existing anisyl-containing anilino pyrimidine derivatives. There is a great increase in stability.
CONDENSED-RING PYRIMIDYLAMINO DERIVATIVE, PREPARATION METHOD THEREFOR, AND INTERMEDIATE, PHARMACEUTICAL COMPOSITION AND APPLICATIONS THEREOF
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Paragraph 0164; 0165, (2018/03/25)
Disclosed are a condensed-ring pyrimidylamino derivative, a preparation method therefor, and an intermediate, a pharmaceutical composition and applications thereof. The method for preparing the condensed-ring pyrimidylamino derivative comprises: in a solvent, in the presence of a palladium-containing catalyst, allowing a compound represented by formula I-a and a compound represented by formula I-b' to have a coupling reaction, and then preparing a compound represented by formula I by means of a deprotection reaction. Also disclosed applications of the condensed-ring pyrimidylamino derivative in the preparation of drugs for preventing, relieving and/or treating tumors or diseases caused by an anaplastic lymphoma kinase. The condensed-ring pyrimidylamino derivative of the present invention has an obvious restraint effect on the anaplastic lymphoma kinase.
Preparation method of 2-isopropoxy-5-methyl-4-(piperidine-4-yl) aniline dihydrochloride
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Paragraph 0026; 0027; 0028, (2017/08/29)
The invention relates to a preparation method of 2-isopropoxy-5-methyl-4-(piperidine-4-yl) aniline dihydrochloride. The preparation method comprises the following steps: carrying out a nucleophilic substitution reaction, a coupling reaction and a reduction reaction by taking 1-chloro-5-fluoro-2-methyl-4-nitrobenzene as a starting material so as to obtain 1-benzyl-4-(5-isopropoxy-2-methyl-4-nitrophenyl)-1,2,3,6-tetrahydropyridine; carrying out a reduction reaction on the 1-benzyl-4-(5-isopropoxy-2-methyl-4-nitrophenyl)-1,2,3,6-tetrahydropyridine again to obtain the 2-isopropoxy-5-methyl-4-(piperidine-4-yl) aniline dihydrochloride. The method does not use catalysts such as platinum and rhodium, is simple and convenient in reaction technology and high in yield, avoids the high pressure reaction condition of the existing process, improves the safety, and shortens the reaction time, thus being suitable for mass production.