1055943-40-2Relevant articles and documents
Preparation method of neratinib
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Page/Page column 10-11, (2019/11/04)
The invention relates to a preparation method of neratinib. The preparation method specifically comprises the steps: (1) in an organic solvent 1, trans-4-dimethylaminocrotonic acid hydrochloride and achloride agent react, and thus a solution containing (e)-4-(dimethylamino)but-2-enoyl chloride (hydrochloride) is obtained; (2) a solution of an organic solvent 2 containing 6-amino-4-[[3-chloro-4-[(pyridine-2-yl)methoxy]phenyl]amino]-3-cyano-7-ethoxyquinoline is added into the solution obtained in the step (1) to react, and then neratinib hydrochloride is obtained; and (3) the neratinib hydrochloride obtained in the step (2) is mixed with water and an organic solvent 3, a reaction is carried out after the pH value is regulated to be 7-10, and then the neratinib is obtained. The synthesis method has the advantages that the yield is high, the product purity is high, the production cost is low, operation is safe, easy and convenient, and large-scale industrial production is easy.
A arab league law for nepal analogue and its preparation and use (by machine translation)
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Paragraph 0075; 0076, (2019/01/10)
The invention discloses a arab league law for nepal analogs, shown as formula I. In addition, also discloses a high purity of the preparation method of the analogue, trans - 4 - dimethylamino crotonic acid hydrochloride as the raw material, in thionyl chl
QUINAZOLINE DERIVATIVE, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION AND APPLICATION THEREOF
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Paragraph 0134; 0138, (2017/07/14)
Disclosed are a quinazoline derivative, a preparation method therefor, and a pharmaceutical composition and an application thereof. The present invention provides a compound represented by general formula I, a stereoisomer thereof and a pharmaceutical acceptable salt or a solvate thereof. The quinazoline derivative of the present invention has a unique chemical structure, is characterized by irreversibly inhibiting EGFR tyrosine kinase, has high biological activity, apparently improves the inhibiting effect on the EGFR tyrosine kinase, has quite strong tumor inhibiting effect on tumor cells and a transplantation tumor pathological model of animal tumors, and has good market developing prospects.
Preparation method for afatinib
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Paragraph 0035; 0036; 0037, (2016/10/08)
The invention provides a preparation method for afatinib. The preparation method comprises the following steps: subjecting trans-4-dimethylaminocrotonic acid hydrochloride (III) to chlorination so as to obtain trans-4-dimethylaminocrotonyl chloride hydrochloride (IV); and reacting the compound (IV) with N4-(3-chloro-4-fluoro-phenyl)-7-((S)-tetrahydrofuran-3-yl-oxy)quinazoline-4,6-diamine (V) so as to prepare afatinib (VI). Reaction equations are described in the specification.
Method for purifying neratinib
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Paragraph 0032; 0034-0035, (2017/04/14)
The invention relates to a method for purifying neratinib. The method provided by the invention is capable of effectively reducing the content of impurities in neratinib and preparing high-purity neratinib, and moreover is simple in operation, high in yield and very applicable to industrial production.
PROCESS FOR THE MANUFACTURE OF (E)-4-N,N-DIALKYLAMINO CROTONIC ACID IN HX SALT FORM AND USE THEREOF FOR SYNTHESIS OF EGFR TYROSINE KINASE INHIBITORS
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, (2015/07/16)
The present invention is directed to an efficient process for the manufacture of (E)-4-N,N- dialkylamino crotonic acid in HX salt form of formula I, wherein R1 and R2 independently denote C1-3-alkyl groups and Xˉ denotes an acid anion, such as the chloride, bromide, tosylate, mesylate or trifluoroacetate anion, with high quality, and a process for synthesis of EGFR tyrosine kinase inhibitors with heterocyclic quinazoline, quinoline or pyrimidopyrimidine core structure, using the acid addition salt I and activated derivatives thereof as intermediates.
PROCESS FOR THE MANUFACTURE OF (E)-4-N,N-DIALKYLAMINO CROTONIC ACID IN HX SALT FORM AND USE THEREOF FOR SYNTHESIS OF EGFR TYROSINE KINASE INHIBITORS
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, (2015/07/15)
The present invention is directed to an efficient process for the manufacture of (E)-4-N,N-dialkylamino crotonic acid in HX salt form of formula I wherein R1 and R2 independently denote C1-3-alkyl groups and X? denotes an acid anion, such as the chloride, bromide, tosylate, mesylate or trifluoroacetate anion, with high quality, and a process for synthesis of EGFR tyrosine kinase inhibitors with heterocyclic quinazoline, quinoline or pyrimidopyrimidine core structure, using the acid addition salt I and activated derivatives thereof as intermediates.
QUINAZOLINE DERIVATIVES SUBSTITUTED BY ANILINE, PREPARATION METHOD AND USE THEREOF
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Paragraph 0212; 0213, (2013/07/25)
The invention relates to quinazoline derivatives substituted by aniline which are represented by the below formula (I), pharmaceutical acceptable salts and stereoisomer thereof, wherein these groups of R1, R2, R3, R4, R5, R6, L and n have the meanings given in the specification. The invention also relates to preparation methods, pharmaceutical compositions, pharmaceutical preparation and the use for preparation of medicine of treating excessive hyperplasia and chronic obstructive pulmonary disease and uses for treating excessive hyperplasia and chronic obstructive pulmonary disease thereof.
QUINAZOLINE DERIVATIVES SUBSTITUTED BY ANILINE, PREPARATION METHOD AND USE THEREOF
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Paragraph 0276; 0277, (2013/07/25)
The invention relates to quinazoline derivatives substituted by aniline which are represented by the below formula (I), pharmaceutical acceptable salts and stereoisomer thereof, wherein these groups of R1, R2, R3, R4, R5, R6, L and n have the meanings given in the specification. The invention also relates to preparation methods, pharmaceutical compositions, pharmaceutical preparation and the use for preparation of medicine of treating excessive hyperplasia and chronic obstructive pulmonary disease and uses for treating excessive hyperplasia and chronic obstructive pulmonary disease thereof.
IMPROVED PROCESS FOR PREPARATION OF COUPLED PRODUCTS FROM 4-AMINO-3-CYANOQUINOLINES USING STABILIZED INTERMEDIATES
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Page/Page column 9-10, (2010/05/13)
This invention discloses improved methods for coupling a 4-(amino)-2-butenoyl group to an amino group at the 6- or 7-position of a 4-amino-3-quinolinecarbonitrile by generating a stabilized 4-(amino)-2-butenoyl chloride hydrochloride.
