69249-22-5Relevant articles and documents
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
(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.
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.