- Method for synthesizing 2-amino-3-chloro-5-trifluoromethylpyridine
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The invention discloses a method for synthesizing 2-amino-3-chloro-5-trifluoromethylpyridine, and belongs to the technical field of organic synthesis. Specifically, starting from 2-aminopyridine, three chemical reactions of bromination, chlorination and coupling are involved, and two organic solvents are used in the whole process; and after the three-step reaction, recrystallization treatment is carried out to obtain the high-purity 2-amino-3-chloro-5-trifluoromethylpyridine. The method is mild in reaction condition and easy to control, and the obtained product is high in purity; reaction rawmaterials and organic solvents are easy to obtain and low in price, and a new way is provided for large-scale production.
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Paragraph 0007; 0020; 0022; 0026; 0028; 0032; 0034
(2021/02/06)
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- Directing Group Enables Electrochemical Selectively Meta-Bromination of Pyridines under Mild Conditions
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Without the use of catalysts and oxidants, a facile and sustainable electrochemical bromination protocol was developed. By introducing the directing groups, the regioselectivity of pyridine derivatives could be controlled at themeta-position utilizing the inexpensive and safe bromine salts at room temperature. A variety of brominated pyridine derivatives were obtained in 28-95% yields, and the reaction could be readily performed at a gram scale. By combining the installation and removing the directing group, the concept ofmeta-bromination of pyridines could be verified.
- Wu, Yanwei,Xu, Shanghui,Wang, Hong,Shao, Dongxu,Qi, Qiqi,Lu, Yi,Ma, Li,Zhou, Jianhua,Hu, Wei,Gao, Wei,Chen, Jianbin
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p. 16144 - 16150
(2021/07/19)
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- DIARYLTHIOHYDANTOIN COMPOUND AS ANDROGEN RECEPTOR ANTAGONIST
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The present application belongs to the field of medicine. In particular, the present application relates to a diarylthiohydantoin compound as an androgen receptor antagonist or a pharmaceutically acceptable salt thereof, a preparation method of the same, a pharmaceutical composition comprising the compound, and a use thereof in treating a cell proliferative disease mediated by androgen. The compound of the present application has good antagonistic effect on androgen receptor and exhibits excellent antitumor effect.
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Paragraph 0804-0806
(2020/07/07)
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- HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS
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Disclosed are compounds of Formula (I'), methods of using the compounds to modulate PD-1/PD-L1 interaction, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or viral infections.
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Page/Page column 72
(2017/08/01)
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- Design, synthesis, and biological evaluation of novel imidazo[1,2-a]pyridine derivatives as potent c-met inhibitors
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A series of imidazo[1,2-a]pyridine derivatives against c-Met was designed by means of bioisosteric replacement. In this study, a selective, potent c-Met inhibitor, 22e was identified, with IC50 values of 3.9 nM against c-Met kinase and 45.0 nM
- Li, Chunpu,Ai, Jing,Zhang, Dengyou,Peng, Xia,Chen, Xi,Gao, Zhiwei,Su, Yi,Zhu, Wei,Ji, Yinchun,Chen, Xiaoyan,Geng, Meiyu,Liu, Hong
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supporting information
p. 507 - 512
(2015/05/27)
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- COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF PARASITIC DISEASES
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The present invention provides compounds of formula I: [INSERT FORMULA HERE] or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a Plasmodium parasite, such as malaria.
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Page/Page column 93
(2014/06/11)
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- A mild method for the regioselective bromination of 2-aminopyridines
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An efficient and regioselective bromination of 2-aminopyridines was developed. The environmental friendly bromination occurs under mild and clean conditions using readily available 1-butylpyridinium bromide as the bromine source and hydrogen peroxide as the green oxidant.
- Xu, Tong,Zhou, Wen,Wang, Jing,Li, Xue,Guo, Jun-Wen,Wang, Bin
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supporting information
p. 5058 - 5061
(2015/01/08)
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- QUINOLONE COMPOUND
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The present invention provides a compound represented by the formula (I) wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R1 is (1) cyclopropyl optionally substituted by 1 to 3 halogen atoms or (2) phenyl optional
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Paragraph 0842
(2014/07/08)
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- QUINOLONE COMPOUND
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The present invention provides a compound represented by the formula (I) wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R1 is (1) cyclopropyl optionally substituted by to 3 halogen atoms or (2) phenyl optionally
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Page/Page column 87; 88
(2013/03/28)
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- BIARYL COMPOUNDS AND METHODS OF USE THEREOF
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Provided herein are compounds for treatment of KIT, CSF-1R and/or FLT3 kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
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Page/Page column 213
(2011/04/13)
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- FLUOROISOQUINOLINE SUBSTITUTED THIAZOLE COMPOUNDS AND METHODS OF USE
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The invention relates to thiazole compounds of Formula (I) and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein. The invention also relates to the therapeutic use of such thiazole compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.
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Page/Page column 143-144
(2010/08/08)
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- HETEROARYLOXY QUINAZOLINE DERIVATIVE
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Disclosed are compounds of the following formula and their pharmaceutically-acceptable salts, which have an effect of glucokinase activation and are useful in the field of medicines for treatment for diabetes, obesity, etc. (wherein ring A represents a pyrazolyl group optionally having a lower alkyl group, etc.; ring B represents a heteroaryl group; R represents a lower alkyl group, etc.; R1 represents a group of a formula: (wherein R11 and R12 each independently represent a hydrogen atom, etc.; m indicates an integer of from 2 to 6), etc.; R2 represents a lower alkyl group, etc.; r indicates an integer of from 0 to 3; k indicates an integer of from 0 to 4).
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Page/Page column 45-46
(2010/09/05)
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- 2-CARBOXY THIOPHENE DERIVATIVES AS ANTI VIRAL AGENTS
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Anti-viral agents of compounds of Formula (I): wherein A, R1, R2 and R3 are as defined in the specification, processes for their preparation and their use in HCV treatment are provided.
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Page/Page column 95-96
(2008/12/05)
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- 5-HETEROARYL THIAZOLES AND THEIR USE AS P13K INHIBITORS
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The invention provides thiazole derivatives of formula (I), or pharmaceutically acceptable salts thereof in which Ring A, R1, R2 and R3 are as defined in the specification; a processes for their preparation; pharmaceutical compositions containing them; and their use in therapy, for example in the treatment of disease mediated by a PI3K enzyme and/or a mTOR kinase.
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Page/Page column 127
(2010/11/30)
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- Halogenation of pyridinium-N-(2'-pyridyl)aminide: An easy synthesis of halo-2-aminopyridines
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The regioselective halogenation of pyridinium-N-(2'-pyridyl)aminide 1 with N-chloro, bromo or iodosuccinimide under mild conditions is described. The method, combined with a reduction of the N-N bond, allows an easy preparation of 5-halo and 3,5-dihalo-2-aminopyridines 4.
- Burgos,Delgado,Garcia-Navio,Izquierdo,Alvarez-Builla
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p. 8649 - 8654
(2007/10/02)
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- Process for the production of 2-amino-3-hydroxypyridine derivatives
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2-Amino-3-hydroxy-5-chloropyridine and 2-amino-3-hydroxy-5-bromopyridine are produced by selective hydrolysis of corresponding 2-amino-3,5-dihalopyridines.
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