69249-22-5Relevant academic research and scientific papers
C-H-Functionalization of 1,2,4-triazines: Oxidation and elimination pathways of aromatization of σh-adducts
Berezin,Rusinov,Charushin
, p. 1359 - 1363 (2014)
An approach to the synthesis of 1,2,4-triazine thienyl and furyl derivatives through the reaction of aromatic nucleophilic substitution of hydrogen was suggested. Oxidation and cine-elimination pathways of aromatization of the intermediate σH-a
Synthetic Route Design of AZD4635, an A2AR Antagonist
Littleson, Mairi M.,Campbell, Andrew D.,Clarke, Adam,Dow, Mark,Ensor, Gareth,Evans, Matthew C.,Herring, Adam,Jackson, Bethany A.,Jackson, Lucinda V.,Karlsson, Staffan,Klauber, David J.,Legg, Danny H.,Leslie, Kevin W.,Morav?ík, ?tefan,Parsons, Chris D.,Ronson, Thomas O.,Meadows, Rebecca E.
, p. 1407 - 1419 (2019/08/12)
The AstraZeneca approach to synthetic Route Design is exemplified through our AZD4635 chemical development program. The identification of possible new route concepts is presented, as well as their subsequent prioritization for practical exploration based on project objectives. Selected ideas were tested to demonstrate proof of concept for the bond formation strategy and, where successful, were fed into a decision tool based on key SELECTion principles.
(HETERO)ARYLAMIDE COMPOUND FOR INHIBITING PROTEIN KINASE ACTIVITY
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Paragraph 0136; 0137, (2019/10/29)
Provided are a (hetero)arylamide compound as shown in formula (I) having an inhibitory effect on protein kinase activity, a pharmaceutically acceptable salt, a stereoisomer, a solvate or hydrate thereof, a pharmaceutical composition comprising the compound or a derivative thereof, and a method for preparing the compound. The compound can be used as an irreversible inhibitor for protein kinase for preparing a plurality of drugs comprising an anti-tumour drug.
HETEROCYCLIC COMPOUND
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Paragraph 1005; 1006, (2019/06/17)
Provided is a heterocyclic compound that may have a GCN2 inhibitory action, and is expected to be useful for the prophylaxis or treatment of GCN2 associated diseases including cancer and the like. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof.
Improved method for synthetizing lamotrigine
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Paragraph 0043; 0044; 0045, (2018/07/06)
The invention discloses an improved method for synthetizing lamotrigine. The method comprises the following steps: step I, carrying out helogenating reaction through 3-amino-1,2,4-triazine (I) and a halogenating reagent in the presence of an organic solvent to obtain 3-amino 6-halogeno-1,2,4-triazine (II); step II, carrying out amination reaction of a compound II to prepare 3,5-diamino 6-halogeno-1,2,4-triazine (compound III); and step III, carrying out suzuki coupling reaction through the compound III and 2,3-dichlorobenzene boric acid derivative in the solvent under catalysis of palladium/[N,N] pyridine amidino ligand/alkali to prepare lamotrigine (IV). Through the method, metal cyanide is not used; meanwhile, the method is high in reaction selectivity and high in reaction yield.
DIACYLGLYCEROL ACYLTRANSFERASE 2 INHIBITORS
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Page/Page column 49, (2018/03/09)
Compounds of Formula (I) that inhibit the activity of the diacylglycerol acyltransferase 2 (DGAT2) and their uses in the treatment of diseases linked thereto in animals are described herein.
Heteroaryl substituted 1, 2, 4-triazin-3-amine derivative , preparation method and application thereof in medicine
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Paragraph 0416; 0418; 0419; 0420; 0421, (2018/09/26)
The present invention relates to a heteroaryl substituted 1, 2, 4-triazin-3-amine derivative, a preparation method thereof and an application thereof in medicine. In particular, the invention relatesto the heteroaryl substituted 1, 2, 4-triazin-3-amine de
Imidazotriazine and imidazodiazine compounds
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Page/Page column 44, (2017/04/11)
The present invention provides thiazole compounds of Formula I wherein X, Y, Z, X1, X2, X3, X4, X5, R1, R2, R4, R5, R6, R7, and W, are
HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS
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Page/Page column 66-67, (2017/08/01)
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.
The discovery of pyridinium 1,2,4-triazines with enhanced performance in bioconjugation reactions
Siegl, Sebastian J.,Dzijak, Rastislav,Vázquez, Arcadio,Pohl, Radek,Vrabel, Milan
, p. 3593 - 3598 (2017/07/10)
1,2,4-Triazines have recently been identified as versatile dienes participating in the inverse electron-demand Diels-Alder reaction with strained dienophiles. However, their widespread utility in bioconjugation reactions is still limited. Herein, we repor
