5521-58-4Relevant articles and documents
Heterocyclic compound as well as pharmaceutical composition, preparation method, intermediate and application thereof
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, (2021/06/23)
The invention discloses a heterocyclic compound as well as a pharmaceutical composition, a preparation method, an intermediate and application thereof. The structure of the heterocyclic compound is shown as a formula I, and the heterocyclic compound has CDK7 inhibitory activity and can be used for treating diseases such as tumors.
Preparation method, product and application of 2-amino-5-methylpyrazine
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Paragraph 0037; 0046-0048; 0057-0059; 0068-0069, (2020/11/25)
The invention belongs to the field of chemical synthesis, and relates to a preparation method, product and application of 2-amino-5-methylpyrazine. The preparation method comprises the following steps: reacting 2-aminomalonamide with pyruvic aldehyde to generate 2-methyl-5-hydroxy-4-pyrazinamide; enabling 2-methyl-5-hydroxy-4-pyrazinamide to react with phosphorus oxychloride so as to generate 2-methyl-5-chloro-4-cyanopyrazine; carrying out a hydrogenation reaction on the 2-methyl-5-chloro-4-cyanopyrazine to generate 2-methyl-4-cyanopyrazine, and hydrolyzing the 2-methyl-4-cyanopyrazine to obtain 2-methyl-4-amide pyrazine; and carrying out Hofmann degradation on the 2-methyl-4-amide pyrazine so as to obtain the 2-methyl-5-aminopyrazine. The method belongs to a brand-new 2-amino-5-methylpyrazine preparation method, is simple and convenient to operate, high in yield and low in cost, and is suitable for industrial large-scale production.
Synthesis and Characterization of 2-(2-Pyridinyl)pyrazine and 2,2′-Bipyrazine Derivatives
KomReddy, Venugopal,Rillema, D. Paul,Nguyen, Huy,Kadel, Lava
, p. 972 - 979 (2019/02/05)
A convenient and high yield preparation of derivatives of 2-(2-pyridinyl)pyrazine and derivatives of 2,2′-bipyrazine compounds from their derivatives of bromopyrazine using Stille coupling is reported. X-ray structures, elemental analyses, 1H, 13C-NMR, and mass spectral data of the compounds are given.
Use of a Curtius Rearrangement as Part of the Multikilogram Manufacture of a Pyrazine Building Block
Steven, Alan,Hopes, Phillip
, p. 77 - 81 (2018/02/06)
Commercial route definition for a glucokinase activator called for a reevaluation of the synthesis and processes used to access multikilogram quantities of 2-amino-5-methylpyrazine. After consideration of different options, a variation of the Curtius rearrangement used by the medicinal chemistry route was selected for further development. The formation of an acyl azide for the Curtius rearrangement required a process safety control strategy to be put in place. The process developed was used to successfully deliver multikilogram quantities of 2-amino-5-methylpyrazine in an overall yield of 68%, starting from 5-methylpyrazine-2-carboxylic acid.
Multimodal Vacuum-Assisted Plasma Ion (VaPI) Source with Transmission Mode and Laser Ablation Sampling Capabilities
Keelor, Joel D.,Farnsworth, Paul B.,L. Weber, Arthur,Abbott-Lyon, Heather,Fernández, Facundo M.
, p. 897 - 907 (2016/05/02)
We have developed a multimodal ion source design that can be configured on the fly for various analysis modes, designed for more efficient and reproducible sampling at the mass spectrometer atmospheric pressure (AP) interface in a number of different applications. This vacuum-assisted plasma ionization (VaPI) source features interchangeable transmission mode and laser ablation sampling geometries. Operating in both AC and DC power regimes with similar results, the ion source was optimized for parameters including helium flow rate and gas temperature using transmission mode to analyze volatile standards and drug tablets. Using laser ablation, matrix effects were studied, and the source was used to monitor the products of model prebiotic synthetic reactions. [Figure not available: see fulltext.]
NITROGEN-CONTAINING FUSED RING COMPOUNDS AS CRTH2 ANTAGONISTS
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, (2014/10/16)
The present application relates to nitrogen-containing fused ring compounds shown by general formula (I), a pharmaceutically acceptable salt thereof and a stereoisomer thereof as CRTH2 antagonist, wherein X1, X2, X3, X4, X5, W, X, Y, L1, L2, L3, A, B are as defined in the description; the present application further relates to a method for preparing the compounds, a pharmaceutical formulation and a pharmaceutical composition comprising the compounds, a use of the compounds for the manufacture of a medicament for the treatment and/or prevention of diseases related to activity of CRTH2.
Peptide deformylase inhibitors
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Page/Page column, (2014/12/09)
The present invention relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods directed to bacterial infections and inhibition of bacterial peptide deformylase (PDF) activity.
NITROGEN-CONTAINING FUSED RING COMPOUNDS FOR USE AS CRTH2 ANTAGONISTS
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, (2014/11/13)
The present application relates to nitrogen-containing fused ring compounds shown by general formula (I), a pharmaceutically acceptable salt thereof and a stereoisomer thereof as CRTH2 antagonist, wherein X1, X2, X3, X4, X5, W, X, Y, L1, L2, L3, A, B are as defined in the description; the present application further relates to a method for preparing the compounds, a pharmaceutical formulation and a pharmaceutical composition comprising the compounds, a use of the compounds for the manufacture of a medicament for the treatment and/or prevention of diseases related to activity of CRTH2.
PEPTIDE DEFORMYLASE INHIBITORS
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Page/Page column, (2014/02/15)
The present invention relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods directed to bacterial infections and inhi-bition of bacterial peptide deformylase (PDF) activity
TYPE II RAF KINASE INHIBITORS
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, (2011/08/08)
The present invention relates to novel compounds which are able to modulate b-raf kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.