- Synthesizing method of (E)-5-methyl-1H-pyrrolo-[2,3-b] pyridine-3-formaldoxime
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The invention relates to a synthesizing method of (E)-5-methyl-1H-pyrrolo-[2,3-b] pyridine-3-formaldoxime, which solves the technical problem that an effective synthesizing method is not discovered at present. The synthesizing method provided by the invention comprises the following steps: brominating 2-amino-5-picoline, so as to obtain a compound 1; performing a reaction on the compound 1 and trimethylsilylacetylene under a condition of a Sonogashira coupling reaction, so as to generate a compound 2; performing a reaction on the compound 2 and sodium hydride to form a pyrrole ring, so as to generate a compound 3; performing a reaction on the compound 3 and urotropine, so as to generate a compound 4; performing the compound 4, hydroxylamine hydrochloride and sodium acetate, so as to obtain the target product (E)-5-methyl-1H-pyrrolo-[2,3-b] pyridine-3-formaldoxime. As a sodium acetate, the (E)-5-methyl-1H-pyrrolo-[2,3-b] pyridine-3-formaldoxime is widely applied in the pharmaceutical industry.
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Paragraph 0008
(2017/09/02)
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- Exploring the isoform selectivity of TGX-221 related pyrido[1,2-a]pyrimidinone-based Class IA PI 3-kinase inhibitors: Synthesis, biological evaluation and molecular modelling
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A novel series of TGX-221 analogues was prepared and tested for their potency against the p110α, p110β, and p110δ isoforms of the PI3K enzyme, and in two cellular assays. The biological results were interpreted in terms of a p110β comparative model, in order to account for their selectivity towards this isoform. A CH2NH type linker is proposed to allow binding into the specificity pocket proposed to accommodate the high p110β-selectivity of TGX-221, although there was limited steric tolerance for substituents on the pendant ring with the 2-position most favourable for substitution.
- Marshall, Andrew J.,Lill, Claire L.,Chao, Mindy,Kolekar, Sharada V.,Lee, Woo-Jeong,Marshall, Elaine S.,Baguley, Bruce C.,Shepherd, Peter R.,Denny, William A.,Flanagan, Jack U.,Rewcastle, Gordon W.
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supporting information
p. 3796 - 3808
(2015/07/27)
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- Synthesis and study of nucleic acids interactions of novel monomethine cyanine dyes
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Six asymmetric monomethine cyanine dyes have been synthesized and their spectral characteristics and interaction with double stranded (ds)DNA have been investigated for their prospective use as fluorescent markers in molecular biology. Therefore, the non-covalent binding of the compounds with dsDNA was explored. Apart from the fluorescence spectroscopy, the study includes UV/Vis spectrophotometry and circular dichroism spectroscopy, as well as the thermal melting experiments. Although the compounds show relatively low binding affinity toward dsDNA and do not have intrinsic fluorescence, in the presence of dsDNA they exhibited considerable enhancement in fluorescence intensity. Therefore the studied dyes show interesting platform for future modifications directed toward more sequence selective derivatives. The compound with the highest affinity toward dsDNA showed interesting anti-proliferative potential and specificity.
- Kaloyanova, Stefka,Crnolatac, Ivo,Lesev, Nedyalko,Piantanida, Ivo,Deligeorgiev, Todor
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scheme or table
p. 1184 - 1191
(2012/03/27)
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- Synthesis of 5-bromo-6-methyl imidazopyrazine, 5-bromo and 5-chloro-6-methyl imidazopyridine using electron density surface maps to guide synthetic strategy
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Small heteroaromatic rings are valuable monomers in drug discovery that can enable rapid access to novel and desirable chemical space. Installation of a synthetic handle on a heteroaromatic core may be difficult if steric and electronic factors are not in alignment with the desired transformation. Described are practical routes for the construction of 5-bromo-6-methyl imidazopyrazine (1) as well as 5-bromo and 5-chloro-6-methyl imidazopyridines (2a and 2b), which were developed using electron density surface maps encoded with ionization potential to guide synthetic strategy.
- Harris, Anthony R.,Nason, Deane M.,Collantes, Elizabeth M.,Xu, Wenjian,Chi, Yushi,Wang, Zhihan,Zhang, Bingzhi,Zhang, Qingjian,Gray, David L.,Davoren, Jennifer E.
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experimental part
p. 9063 - 9066
(2011/12/03)
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- ADAMANTYL DERIVATES AS P2X7 RECEPTOR ANTAGONISTS
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The invention provides compounds of formula (I) pharmaceutically acceptable salt or solvate thereof, in which R1, A1, m and A are as defined in the specification; a process for their preparation; pharmaceutical compositions containin
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Page/Page column 143-144
(2010/10/20)
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- Substituted pyridines as selective cyclooxygenase-2 inhibitors
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The invention encompasses the novel compound of Formula I as well as a method of treating COX-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. STR1 The invention also encompasses certain pharmaceutical compositions for treatment of COX-2 mediated diseases comprising compounds of Formula I.
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- 2-pyridinyl-3(4-methylsulfonyl)phenylpyridines: Selective and orally active cyclooxygenase-2 inhibitors
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A series of novel 2-pyridinyl-3-(4-methylsulfonyl)phenylpyridines has been synthesized and evaluated with respect to their ability to inhibit the isozymes of cyclooxygenase, COX-1, and COX-2. Optimum COX-2 activity is observed by introduction of a substituent at C5 of the central pyridine. 5- Chloro-3-(4-methylsulfonyl)phenyl-2(2-methyl-5-pyridinyl)pyridine 33 was identified as the optimum compound in this series.
- Friesen, Richard W.,Brideau, Christine,Chan, Chi Chung,Charleson, Stella,Deschenes, Denis,Dube, Daniel,Ethier, Diane,Fortin, Rejean,Gauthier, Jacques Yves,Girard, Yves,Gordon, Robert,Greig, Gillian M.,Riendeau, Denis,Savoie, Chantai,Wang, Zhaoyin,Wong, Elizabeth,Visco, Denise,Xu, Li Jing,Young, Robert N.
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p. 2777 - 2782
(2007/10/03)
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- Total synthesis of dimethyl sulfomycinamate
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The first total synthesis of dimethyl sulfomycinamate (1) is described. Highlights of the synthesis include a selective palladium-catalyzed coupling reaction on the bromotriflate 21, and a condensation reaction to form the oxazole ring.
- Ross Kelly,Lang, Fengrui
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p. 5319 - 5322
(2007/10/02)
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- SYNTHESIS OF THE MUTAGENIC 2-AMINO-1,6-DIMETHYLIMIDAZOPYRIDINE (1,6-DMIP) AND FIVE OF ITS ISOMERS
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Synthetic routes to 2-amino-1,6-dimethylimidazopyridine and its 1,5-, 1,7-, 3,5- 3,6- and 3,7-dimethyl isomers from methyl derivatives of 3-hydroxy- or 2-amino-pyridine and 2-chloronicotinic acid are described.
- Lindstroem, Stefan,Ahmad, Tania,Grivas, Spiros
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p. 529 - 540
(2007/10/02)
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- Bromination of Pyridines. II. Bromination of Aminopicolines
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The bromination of all ten possible aminopicolines 1-10 was investigated.In general, the major brominated product was that corresponding to electrophilic attack at the sites para or ortho to the amino group.
- Dunn, A. D.,Currie, A.,Hayes, L. E.
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p. 369 - 374
(2007/10/02)
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- Herbicidal pyridine compounds
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Herbicidal 3- and/or 5-halogenomethyl-pyrid-2-yloxyphenoxy compounds and processes for making and using the same. Intermediates for making these compounds and their preparation are also disclosed. Thus, for example, 2-chloro-5-trichloromethylpyridine is prepared by a liquid phase chlorination of 3-methylpyridine under the influence of ultra violet light.
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- Herbicidal compounds
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A herbicidal sulphonamide compound of the formula (I): STR1 and salts thereof, wherein R1 is a pyridyl group of the formula: STR2 wherein the group X of the pyridyl group represents a fluorine, chlorine, bromine, or iodine atom, or an alkyl radical of 1 to 4 carbon atoms optionally substituted by one or more fluorine or chlorine atoms, and the group Y represents hydrogen, fluorine chlorine, bromine, or iodine or an alkyl radical of 1 to 4 carbon atoms optionally substituted by one or more fluorine or chlorine atoms; R2 represents an alkyl radical of 1 to 6 carbon atoms optionally substituted by one or more fluorine atoms; and R3 is hydrogen or an alkyl radical of 1 to 4 carbon atoms.
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- Herbicidal mono- or di-substituted-2-pyridinyloxy-phenoxy-lower-alkane-carbamates
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Herbicidal pyridine compounds of the formula (I): STR1 wherein Z may be halogen, or a fluorine- or chlorine-substituted alkyl group of 1 to 4 carbon atoms, and Y may be hydrogen, halogen, or a fluorine- or chlorine-substituted alkyl group of 1 to 4 carbon atoms; X may be an OH group or an acyloxy group; a halogen atom; an amino group, a mono- or di-alkyl amino group, or an alkanoylamido group; an alkoxy group optionally substituted by hydroxy or alkoxy; or a mercapto group, an alkylthio group, or a phenylthio group. The invention also provides herbicidal compositions containing the compounds, and processes for making the compounds.
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