- Method for preparing 5-trifluoromethyl uracil
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The invention belongs to the field of organic synthesis, and specifically relates to a method for preparing 5-trifluoromethyl uracil. The method comprises the following steps: firstly, carrying out chlorination reaction on 5-iodouracil and phosphorus oxychloride, thus obtaining 2,4-dichloro-5-iodopyrimidine; secondly, carrying out trifluoromethylation reaction on the 2,4-dichloro-5-iodopyrimidineand a trifluoromethylating reagent, thus obtaining 2,4-dichloro-5-trifluoromethylpyrimidine; finally, enabling the 2,4-dichloro-5-trifluoromethylpyrimidine to react with acetic acid, thus obtaining aproduct. According to the method disclosed by the invention, since chlorination reaction, trifluoromethylation reaction and hydrolysis reaction are adopted, a key intermediate-trifluoromethyl uracil of trifluorothymidine is synthesized in high yield, low cost and low pollution.
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Paragraph 0036-0037
(2019/06/05)
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- Pyrimidine or triazine derivative, and preparation method and use thereof
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The invention relates to an arylaminopyrimidine or triazine derivative, and a preparation method, a medicinal composition and a use thereof, and concretely relates to a compound represented by formula I, or a pharmaceutically acceptable salt or a solvate thereof. In the formula I, R1 to R7, X and Y are defined in the description and claims. The invention also relates to a preparation method of the compound of formula I, the medicinal composition containing the compound, and the pharmacy use of the compound and the medicinal composition. The compound of formula I is an effective tyrosine kinase irreversible inhibitor, and especially has a strong inhibition effect on EGFR-T790M drug-resistant tumors.
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Paragraph 0136; 0137
(2016/10/08)
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- 2,4-Pyrimidinediamine Compounds and Their Uses
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The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
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Paragraph 0313; 0315
(2015/11/10)
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- Trifluoroethoxy group as a leaving group for regioselective sequential substitution reactions of 5-trifluoromethylpyrimidine derivative with heteroatom nucleophiles
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Highly regioselective substitution reaction of 2,4-bis(2,2,2-trifluoroethoxy)-5-(trifluoromethyl)pyrimidine (TFEFP) with aniline derivatives smoothly proceeded firstly at the 2-postion. For the subsequent nucleophilic substitution at the 4-position with alkoxides, trifluoroethoxy group at the 4-position serves as a practically efficient leaving group.
- Kagawa, Takumi,Shigehiro, Daiki,Kawada, Kosuke
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p. 150 - 158
(2015/11/10)
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- SYNTHESIS OF 2,4-DICHLORO-5-TRIFLUOROMETHYL-PYRIMIDINE
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This invention relates to a novel method for the synthesis of 2,4-dichloro-5-trifluoromethyl-pyrimidine useful as intermediate in the manufacture of pharmaceutically active ingredients.
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Paragraph 0060; 0061; 0062; 0063; 0064
(2014/05/20)
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- NOVEL PROCESS FOR THE MANUFACTURE OF 2,4-DICHLORO-5-TRIFLUOROMETHYL-PYRIMIDINE
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This invention relates to a novel method for the synthesis of 2,4-dichloro-5-trifluoromethyl- pyrimidine useful as intermediate in the manufacture of pharmaceutically active ingredients.
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Page/Page column 9-10
(2014/06/11)
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- PYRIMIDINE DERIVATIVES FOR THE TREATMENT OF ABNORMAL CELL GROWTH
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The present invention relates to salts, solvates and substoichiometric solvates of N-[3-[[[2-[(2,3-dihydro-2-oxo-1H-indo1-5-yl)amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]methyl]-2-pyridinyl]-N-methylmethanesulfonamide. The invention also provides pharmaceutical compositions comprising such complexes, as well as methods of treating abnormal cell growth by administering the complexes of the invention.
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Page/Page column 8
(2011/02/26)
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- 2,4-DIAMINOPYRIMIDINE DERIVATES AS PTK2- INHIBITORS FOR THE TREATMENT OF ABNORMAL CELL GROWTH
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The present invention encompasses compounds of general formula (1) wherein R1-R3 and n are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a medicament having the above-mentioned properties.
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Page/Page column 29
(2010/06/15)
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- SUBSTITUTED PYRIMIDINES FOR THE TREATMENT OF CANCER
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The present invention encompasses compounds of general formula (1) wherein B, R1 to R5, Rx, m and n are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use in such treatment.
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Page/Page column 29-30
(2010/10/03)
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- 2, 4 -DIAMINOPYRIMIDINES FOR THE TREATMENT OF DISEASES CHARACTERISED BY EXCESSIVE OR ABNORMAL CELL PROLIFERATION
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The present invention encompasses compounds of general formula (1), wherein A, B, R1 to R5, Rx m, n and p are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain such compounds and the use thereof [as] medicaments.
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Page/Page column 34
(2010/12/26)
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- 2,4-DIAMINOPYRIMIDINE DERIVATIVES USEFUL AS INHIBITORS OF AURORA KINASE
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A 2,4-diaminopyrimidine derivative of the formula (I), or a pharmaceutically acceptable salt thereof, formula (I) wherein R1, R2, R3, R4, X and Y are as defined in the specification; together with processes for their preparation; pharmaceutical compositions containing them; and their use in therapy. The compounds are inhibitors of Aurora kinase.
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Page/Page column 43-44
(2009/06/27)
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- New compounds
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The present invention encompasses compounds of general formula (1) wherein R1, R2, R4, X, m, n and p are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a pharmaceutical composition having the above-mentioned properties.
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Page/Page column 8
(2009/07/10)
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- DIAMINOPYRIDINES FOR THE TREATMENT OF DISEASES WHICH ARE CHARACTERISED BY EXCESSIVE OR ANOMAL CELL PROLIFERATION
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The present invention encompasses compounds of general formula (1) wherein A, B, R1- R3, Rx and n are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a medicament having the above-mentioned properties.
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Page/Page column 22-23
(2009/07/17)
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- NEW COMPOUNDS
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The present invention encompassescompounds of general formula (1) wherein R1 to R4 , X and n are defined as in claim 1, which are suitable for the treatment of ailments characterised byexcessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.
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Page/Page column 13
(2008/12/06)
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- Non-nucleoside reverse transcriptase inhibitors
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The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein R1, R2, R3, R4, R5a, R5b, R6a, R6b and X are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.
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Page/Page column 26; 27
(2008/12/06)
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- 2,4-diamino-pyrimidines as aurora inhibitors
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The present invention encompasses compounds of general formula (1) wherein R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.
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Page/Page column 10
(2008/06/13)
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- Pyrimidine derivatives for the treatment of abnormal cell growth
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The present invention relates to a compound of the formula 1 wherein R1-R4 are as defined herein. Such novel pyrimidine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.
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Page/Page column 43
(2008/06/13)
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- Pyrimidine derivatives for the treatment of abnormal cell growth
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The present invention relates to a compound of the formula 1 or a pharmaceutically acceptable salt, solvate, hydrate, or prodrug thereof, wherein R1-R4 and Ar are as defined herein. Such novel pyrimidine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.
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Page/Page column 29
(2010/02/14)
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- Pyrimidine derivatives for the treatment of abnormal cell growth
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The present invention relates to a compound of the formula 1 wherein A and Ar are as defined herein. Such novel pyrimidine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.
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Page/Page column 20
(2010/02/14)
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- SELECTIVE SYNTHESIS OF CF3-SUBSTITUTED PYRIMIDINES
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The present invention relates to a method of making a compound of the formula (I),wherein X1, X2 and R3-R4 are as defined herein. The method includes reacting a compound of the formula (II) with an amine of formula (III) (HNR33R44) in the presence of a Lewis Acid and a non-nucleophilic base. The 2,4-diamino pyrimidine moiety is a common component in a variety of biologically active drug-like molecules and pyrimidine derivatives have been found to be useful in the 10 treatment of abnormal cell growth, such as cancer, in mammals.
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Page/Page column 9
(2008/06/13)
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- CHK-, PDK- AND AKT-INHIBITORY PYRIMIDINES, THEIR PRODUCTION AND USE AS PHARMACEUTICAL AGENTS
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This invention relates to pyrimidine derivatives of general formula (I) as inhibitors of kinases, their production as well as their use as medications for treating various diseases.
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- Fluorination agent and preparation and use of same
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The invention disclose a hydrogen fluoride containing composition comprising hydrogen fluoride and a compound which is liquid in the standard state (25° C., 1 atmosphere) and has a boiling point of 120° C. or more and pka of 12 or more at 25° C., and use of the composition for a fluorination agent. The compound which can be preferably used is represented by the formula (1): wherein R1 to R4 are a substituted or unsubstituted alkyl or aryl group and can be the same or different, and R1 or R2 or R3 and R4 can bond to form a ring having a nitrogen atom or a nitrogen atom and other hetero atom, or R1 and R3 can bond to form a ring having a nitrogen atom or a nitrogen atom and other hetero atom. The fluorination agent of the invention exerts effect with a similar reaction mechanism to hydrogen fluoride, can be applied to the halogen exchange reaction of a halogen containing organic compound, and can produce a fluorine containing compound with safety and ease without specific equipment or technique.
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