- Preparation method 2 - methyl -5 -bromopyrimidine
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The invention specifically discloses a preparation method of 2 - methyl -5 -bromopyrimidine, and belongs to the technical field of organic synthesis. The method comprises the following steps: a) taking 2 - amino -5 -bromopyrimidine as a raw material, carrying out diazotization reaction or Schedman reaction or 2 - hydroxyl -5 -bromopyrimidine as a raw material to obtain 2 -halo -5 -bromopyrimidine through a halogenated reagent. b) The carboxylic diester is substituted with 2 - halo -5 - bromopyrimidine to give 2-position substituted product. c) The last 2 -bit substituted product is reacted under basic, high temperature conditions to give 2 - methyl -5 - bromopyrimidine. The method has the advantages of easily available raw materials, low cost, simple flow and potential industrial amplification prospect.
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Paragraph 0031-0033
(2021/11/26)
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- SUBSTITUTED DIARYLAMINES AND USE OF SAME AS ANTIOXIDANTS
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The present invention relates to substituted heteroaromatic dianlamine compounds of Formula I and II, their pharmaceutically acceptable salts, and compositions thereof useful as antioxidants, wherein each of X, Y and Z are independently a carbon or nitrogen atom; R1 and R2 are each independently a hydrogen or an electron donating group, but are not both hydrogen, and wherein R1 and R2 are each bonded to a carbon atom in their own respective aryl ring.
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Page/Page column 45-46
(2013/02/28)
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- Preparation of highly reactive pyridine- and pyrimidine-containing diarylamine antioxidants
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We recently reported a preliminary account of our efforts to develop novel diarylamine radical-trapping antioxidants (Hanthorn, J. J. et al. J. Am. Chem. Soc. 2012, 134, 8306-8309) wherein we demonstrated that the incorporation of ring nitrogens into diphenylamines affords compounds which display a compromise between H-atom transfer reactivity to peroxyl radicals and stability to one-electron oxidation. Herein we provide the details of the synthetic efforts associated with that report, which have been substantially expanded to produce a library of substituted heterocyclic diarylamines that we have used to provide further insight into the structure-reactivity relationships of these compounds as antioxidants (see the accompanying paper, DOI: 10.1021/jo301012x). The diarylamines were prepared in short, modular sequences from 2-aminopyridine and 2-aminopyrimidine wherein aminations of intermediate pyri(mi)dyl bromides and then Pd-catalyzed cross-coupling reactions of the amines and precursor bromides were the key steps to yield the diarylamines. The cross-coupling reactions were found to proceed best with Pd(η3-1-PhC3H 4)(η5-C5H5) as precatalyst, which gave higher yields than the conventional Pd source, Pd2(dba) 3.
- Hanthorn, Jason J.,Valgimigli, Luca,Pratt, Derek A.
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experimental part
p. 6908 - 6916
(2012/10/08)
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- HEPATITIS C VIRUS INHIBITORS
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The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts thereof, to compositions containing such compounds and to the use of such compounds as inhibitors of HCV replication.
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Page/Page column 115
(2011/02/24)
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- A simple Cu-catalyzed coupling approach to substituted 3-pyridinol and 5-pyrimidinol antioxidants
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(Chemical Equation Presented) A convenient approach to 3-pyridinols and 5-pyrimidinols via a two-step Cu-catalyzed benzyloxylation/catalytic hydrogenation sequence is presented. The corresponding 3-pyridinamines and 5-pyrimidinamines can be prepared in an analogous sequence utilizing benzylamine in lieu of benzyl alcohol. The radical-scavenging ability of these derivatives are preliminarily explored and reveal that the increased acidities of the pyridinols and pyrimidinols render them susceptible to more significant kinetic solvent effects when compared to phenols.
- Nara, Susheel J.,Jha, Mukund,Brinkhorst, Johan,Zemanek, Tony J.,Pratt, Derek A.
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supporting information; experimental part
p. 9326 - 9333
(2009/04/06)
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- INDOLES USEFUL IN THE TREATMENT OF INFLAMMATION
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There is provided a compound of formula: (I), wherein X, R1, R2, R3, R4, R5 and R6 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of microsomal prostaglandin E synthase-1 is desired and/or required, and particularly in the treatment of inflammation.
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Page/Page column 84
(2010/02/15)
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- Process for preparing 2,5-dibromopyrimidine
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Process for preparing 2,5-dibromopyrimidine A process for preparing 2,5-dibromopyrimidine comprises reacting 5-bromo-2-chloropyrimidine with a solution of hydrogen bromide in a non-aqueous acid at a temperature of between 0° and 120° C. The process can be carried out at low cost and gives high yields.
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