cas 2924-09-6, 5-BROMO-2-FLUOROANILINE | Articles data

Articles about 2924-09-6Total 17 be found

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Anion ligand promoted selective C-F bond reductive elimination enables C(sp2)-H fluorination
A detailed mechanism study on the anion ligand promoted selective C-H bond fluorination is reported. The role of the anion ligand has been clarified by experimental evidence and DFT calculations. Moreover, the nitrate promoted C-F bond reductive elimination enabled a selective C-H bond fluorination of various symmetric and asymmetric azobenzenes to access diverse o-fluoroanilines.
Mao, Yang-Jie,Luo, Gen,Hao, Hong-Yan,Xu, Zhen-Yuan,Lou, Shao-Jie,Xu, Dan-Qian
supporting information
p. 14458 - 14461
(2019/12/09)

1,3-dibromo-4-fluorobenzene preparation method
The invention discloses an industrial preparation method of 1,3-dibromo-4-fluorobenzene. The industrial preparation method of 1,3-dibromo-4-fluorobenzene comprises the steps that o-fluoronitrobenzeneserves as an initial raw material, and 1,3-dibromo-4-fluorobenzene is synthesized through bromine applying, reduction and diazotization-Sandmeyer three step reactions. The obtained 1,3-dibromo-4-fluorobenzene is yellow oily liquid, the purity is 97.5%, the raw material conversion rates of all steps each reach 100%, and the total recovery of the whole process reaches 52.7%.
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(2019/02/27)

A 3-amino-4-fluorophenylboronic acid synthesis method
The invention discloses a synthetic method for 3-amino-4-fluorophenylboronic acid. The method includes the steps of conducting bromination on o-fluoronitrobenzene, conducting reduction to generate 5-bromo-2-fluoroanil, making 5-bromo-2-fluoroanil and tetrahydroxydiboron react in a coupled mode to generate the product, namely, 3-amino-4-fluorophenylboronic acid. According to the method, raw materials can be easily obtained, and operation is easy and convenient. The method is an appropriate route for preparing 3-amino-4-fluorophenylboronic acid.
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(2016/11/24)

Discovery of selective N-[3-(1-methyl-piperidine-4-carbonyl)-phenyl]-benzamide-based 5-HT1F receptor agonists: Evolution from bicyclic to monocyclic cores
Preclinical experiments and clinical observations suggest the potential effectiveness of selective 5-HT1F receptor agonists in migraine. Identifying compounds with enhanced selectivity is crucial to assess its therapeutic value. Replacement of the indole nucleus in 2 (LY334370) with a monocyclic phenyl ketone moiety generated potent and more selective 5-HT1F receptor agonists. Focused SAR studies around this central phenyl ring demonstrated that the electrostatic and steric interactions of the substituent with both the amide CONH group and the ketone C=O group play pivotal roles in affecting the adopted conformation and thus the 5-HT1F receptor selectivity. Computational studies confirmed the observed results and provide a useful tool in the understanding of the conformational requirements for 5-HT1F receptor agonist activity and selectivity. Through this effort, the 2-F-phenyl and N-2-pyridyl series were also identified as potent and selective 5-HT1F receptor agonists.
Zhang, Deyi,Blanco, Maria-Jesus,Ying, Bai-Ping,Kohlman, Daniel,Liang, Sidney X.,Victor, Frantz,Chen, Qi,Krushinski, Joseph,Filla, Sandra A.,Hudziak, Kevin J.,Mathes, Brian M.,Cohen, Michael P.,Zacherl, Deanna,Nelson, David L.G.,Wainscott, David B.,Nutter, Suzanne E.,Gough, Wendy H.,Schaus, John M.,Xu, Yao-Chang
p. 4337 - 4341
(2015/11/03)

CYCLOPROPANECARBOXAMIDO-SUBSTITUTE AROMATIC COMPOUNDS AS ANTI-TUMOR AGENTS
Provided are cyclopropanecarboxamido-substituted aromatic compounds that inhibit protein kinases and their use in anti-tumor area. In particular, tyrosine-kinase inhibitors and Raf-kinase inhibitors as anti-tumor agents, their preparation, pharmaceutical composition, and their use in the treatment of cancer are also provided.
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Paragraph 0282; 0283

(2015/07/22)

Selective reduction of halogenated nitroarenes with hydrazine hydrate in the presence of Pd/C
A large variety of halogenated nitroarenes have been selectively reduced with hydrazine hydrate in the presence of Pd/C to give the corresponding (halogenated) anilines in good yield.
Li, Fang,Frett, Brendan,Li, Hong-Yu
p. 1403 - 1408
(2014/06/23)

CYCLOPROPANECARBOXAMIDO-SUBSTITUTE AROMATIC COMPOUNDS AS ANTI-TUMOR AGENTS
Provided are cyclopropanecarboxamido-substituted aromatic compounds that inhibit protein kinases and their use in anti-tumor area. In particular, tyrosine-kinase inhibitors and Raf-kinase inhibitors as anti-tumor agents, their preparation, pharmaceutical composition, and their use in the treatment of cancer are also provided.
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Page/Page column 58

(2014/01/17)

2-Pyrimidinyl Pyrazolopyridine ErbB Kinase Inhibitors
The present invention provides 2-pyrimidinyl pyrazolopyridine compounds, compositions containing the same, as well as processes for the preparation and their use as pharmaceutical agents.
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Page/Page column 55; 80

(2009/06/27)

2-Pyrimidinyl Pyrazolopyridine Erbb Kinase Inhibitors
The present invention provides 2-pyrimidinyl pyrazolopyridine compounds, compositions containing the same, as well as processes for the preparation and their use as pharmaceutical agents.
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Page/Page column 96; 112

(2008/06/13)

METHODS FOR PREPARING INDAZOLE COMPOUNDS
The invention relates to methods for preparing compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof. Compounds of the formula (I) are useful as anti-angiogenesis agents and as agents for modulating and/or inhibiting the activity of protein kinases, thus providing treatments for cancer or other diseases associated with cellular proliferation mediated by protein kinases.
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Page/Page column 32

(2010/11/30)

PYRIDYL DERIVATIVES AND THEIR USE AS MGLU5 RECEPTOR ANTAGONISTS
The present invention is directed toward pyridyl derivatives of formula (I) as antagonists of the mGlu5 receptor. As such the compounds may be useful for treatment or prevention of disorders remedied by antagonism of the mGlu5 receptor, wherein Ar is phenyl or napthyl each of which may be substituted by one or more C1-C4 alkyl, C1-C4 alkoxy, C1-C5 acyl, halo, amino, nitro, cyano, hydroxy, C1-C5 acylamino, C1-C4 alkylsulfonylamino, mono-, di- or trifluorinated C1-C3 alkyl, substituents which may be the same or different and may bear a CONH2, CONHCH3, CON(CH3)2, CO2H, CO2CH3, OCF3, CH2NHCOCH3, CH2NH2, CH2N(CH3)2, CH2CN, CH2OH, CH2NHSO2CH3, CH2N(CH3)(CH2)2 CN, CH2N(CH3)CH(CH3)2, CH2NHCH(CH3)2, CH2NH(CH2)2CH3, CH2NHCO2R4, CH2NHCH2CH3, CH2NHCH3 NHCOC(CH3)2, or N(S(O)2CH3)2 substituent; R1 is hydrogen, halo, R4, CN, C(NOH)R3, C(NO-R4)R3, (CH)2CO2R4 , (CH2)n OR3 , COR3 , CF3,SR4 , S(O)R4, S(O)2R4, COCH2CO2R3 , NHSO2R4 , NHCOR3, C(NOR3)NH2, CH2OCOR3,(CH2)n NH2, CON(CH3)2 (CH2)nNHCO2R4 , CO2R3, CONH2, CSNH2, C(NH)NHOR3, (CH2)nN(CH3)2, or CONHNHCOR3; R2 is 1,2-ethenediyl or 1,2-ethynediyl; R3 is hydrogen or C1-C4 alkyl; R4 is C1-C4 alkyl; and n is 0, 1, 2,3 or 4; or a pharmaceutically acceptable salt thereof, or an N-oxide thereof.
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Page/Page column 44

(2008/06/13)

TRICYCLIC STEROID HORMONE NUCLEAR RECEPTOR MODULATORS
The present invention relates to methods of treating pathological disorders susceptible to steroid hormone nuclear receptor modulation comprising administering to a patient in need thereof an effective amount of a compound of the formula (I): or a pharmaceutically acceptable salt thereof. In addition, the present invention provides novel pharmaceutical compounds of Formula (I), including the pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions which comprise as an active ingredient a compound of Formula (I).
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Page 171

(2008/06/13)

Discovery of pyrano[3,4-b]indoles as potent and selective HCV NS5B polymerase inhibitors
A novel series of HCV NS5B RNA-dependent RNA polymerase inhibitors containing a pyrano-[3,4-b]indole scaffold is described leading to the discovery of compound 16, a highly potent and selective inhibitor that is active in the replicon system.
Gopalsamy, Ariamala,Lim, Kitae,Ciszewski, Gregory,Park, Kaapjoo,Ellingboe, John W.,Bloom, Jonathan,Insaf, Shabana,Upeslacis, Janis,Mansour, Tarek S.,Krishnamurthy, Girija,Damarla, Murthy,Pyatski, Yelena,Ho, Douglas,Howe, Anita Y. M.,Orlowski, Mark,Feld, Boris,O'Connell, John
p. 6603 - 6608
(2007/10/03)

NITROGENOUS FUSED?RING COMPOUND HAVING PYRAZOLYL GROUP AS SUBSTITUENT AND MEDICINAL COMPOSITION THEREOF
The present invention provides a compound having an excellent inhibitory action on activation of STAT6 and a pharmaceutical composition thereof. Inparticular, it provides a compound represented by the following formula (I), a salt thereof or a hydrate of them. In the formula, X represents a nitrogen-containing condensed aromatic heterocyclic group such as imidazo[1,2-a]pyridine, benzimidazole, quinazoline, quinoline, or 2,1-benzisoxazole and has (R4)n as substituent groups; Y represents a C3-8 cycloalkyl group, C4-8 cycloalkenyl group, 5- to 14-membered non-aromatic heterocyclic group, C6-14 aromatic hydrocarbon cyclic group or 5- to 14-membered aromatic heterocyclic group; n in (R4)n is 0, 1, 2 or 3, and Z groups independently represent (1) hydrogen atom, (2) amino group, (3) halogen atom, (4) hydroxyl group, (5) nitro group, (6) cyano group, (7) azido group, (8) formyl group, (9) hydroxyamino group, (10) sulfamoyl group, (11) guanodino group, (12) oxo group, (13) C2-6 alkenyl group, (14) C1-6 alkoxy group, (15) C1-6 alkylhydroxyamino group, (16) halogenated C1-6 alkyl group, (17) halogenated C2-6 alkenyl group, (18) (i) C3-7cycloalkyl group, (ii) C3-7cycloalkenyl group, (iii) 5- to 14-membered non-aromatic heterocyclic group, each of which may have one or more substituent groups Q, or (19) formula -M1-M2-M3, R1 represents (1) hydrogen atom, (2) halogen atom, (3) hydroxyl group, (4) nitro group, (5) cyano group, (6) halogenated C1-6 alkyl group, (7) C2-6 alkyl group substituted with a hydroxyl or cyano group, (8) C2-6 alkenyl group, or (9) formula -L1-L2-L3, and R2 represents a hydrogen atom or a protecting group; and R3 represents a hydrogen atom, halogen atom, cyano group, amino group, C1-4 alkyl group or halogenated C1-4 alkyl group.
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Page 167; 168

(2008/06/13)

R-ENANTIOMERS OF PYRANOINDOLE DERIVATIVES AGAINST HEPATITIS C
The invention is directed to a compound and a pharmaceutical composition of the formula: Wherein substitutions at R1, R2, R3 - R12, and Y are set forth in the specification.
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Page 27

(2008/06/13)

METHOD FOR THE USE OF PYRANOINDOLE DERIVATIVES TO TREAT INFECTION WITH HEPATITIS C VIRUS
The invention is directed to methods of treating, preventing, or inhibiting a Hepatitis C viral infection in a mammal comprising containing the mammal with an effective amount of a compound of the formula: Wherein substitutions at R1, R2, R3-R12, and Y are set forth in the specification.
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Page 58

(2008/06/13)

Syntheses of Sulfonated Derivatives of 2-Fluoroaniline
Synthesis of 4-amino-3-fluorobenzenesulfonic acid (3) was achieved in two ways: reaction of 2-fluoroaniline (1) with amidosulfonic acid and by first conventionally converting 4-nitro-3-fluoroaniline (8) to 4-nitro-3-fluorobenzenesulfonyl chloride (9) followed subsequently by hydrolysis to 3-fluoro-4-nitrobenzenesulfonic acid (10) and reduction.Hydrogenolysis of 3 gave sulfanilic acid (7).Both, sulfonation of fluorobenzene (6) to 4-fluorobenzenesulfonic acid (11) followed by nitration and sulfonation of 1-fluoro-2-nitrobenzene (12) led to 4-fluoro-3-nitrobenzenesulfonic acid (13).Reduction of 13 gave the isomeric 3-amino-4-fluorobenzenesulfonic acid (4), which was also obtained both by sulfonation of 1 and by sulfonation of o-fluoroacetanilide (14) followed by hydrolysis.Selective hydrogenolyses of 2-amino-5-bromo-3-fluorobenzenesulfonic acid (15), prepared by reaction of 4-bromo-2-fluoroaniline (16) with amidosulfonic acid, and of 4-amino-2-bromo-5-fluorobenzenesulfonic acid (20), obtained by sulfonation of 5-bromo-2-fluoroaniline (19) yielded the isomers 2-amino-3-fluorobenzenesulfonic acid (5) and 3, respectively.The fourth isomer, 3-amino-2-fluorobenzenesulfonic acid (2), was synthesized by sulfur dioxide treatment of the diazonium chloride derived from 2-fluoro-3-nitroaniline (21) to 2-fluoro-3-nitrobenzenesulfonyl chloride (22), followed by hydrolysis to 2-fluoro-3-nitrobenzenesulfonic acid (23) and final Bechamp-reduction.
Courtin, Alfred
p. 68 - 75
(2007/10/02)