122025-09-6Relevant articles and documents
Selective α-deuteration of amines and amino acids using D2O
Chatterjee, Basujit,Krishnakumar, Varadhan,Gunanathan, Chidambaram
, p. 5892 - 5895 (2016)
Monohydrido-bridged ruthenium complex [{(η6-p-cymene)RuCl}2(μ-H-μ-Cl)] catalyzes (catalyst load: 0.5-1 mol %) α-selective deuteration of primary and secondary amines, amino acids, and drug molecules using deuterium oxide (D2O) as a deuterium source. Mechanistic investigations revealed N-H activation of amines, which was also established by single-crystal X-ray analysis of an intermediate. β-Hydride elimination on amide ligand results in formation of imine-ligated ruthenium intermediate and subsequent 1,3-deuteride migrations to imine ligand leading to the selective deuteration at the α-CH2 protons of amine functionality is proposed.
PYRIMIDINE OR PYRIDINE COMPOUNDS, PREPARATION METHOD THEREFOR AND PHARMACEUTICAL USES THEREOF
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Paragraph 0438-0439, (2017/09/19)
The present invention disclosed a class of pyrimidine or pyridine compounds, pharmaceutically acceptable salts, stereoisomers, prodrugs and solvates thereof, preparation method therefor and pharmaceutical compositions and pharmaceutical uses thereof. The compounds can inhibit the variants of EGFR (Epidermis Growth Factor Receptor) proteinases, and therefore can inhibit the growth of a variety of tumor cells effectively. The compounds can be used to prepare antitumor drugs, used for the treatment, combined therapy or prevention of various different cancers. The compounds can overcome the drug resistance induced by the existing first-generation EGFR inhibitors such as gefitinib, erlotinib and so on. Particularly, the compounds can be used to prepare drugs for treating or preventing diseases, disturbances, disorders or conditions mediated by epidermis growth factor receptor variants (such as L858R activated mutants, Exon19 deletion activated mutants and T790M resistant mutants).
Catalytic N-Dealkylation of Tertiary Amines--A Biomimetic Oxygenation Reaction
Chaudhuri, Naba K.,Servando, Ofelia,Markus, Bohdan,Galynker, Igor,Sung, Ming-Sang
, p. 899 - 903 (2007/10/02)
A heterogeneous catalyst system is described for N-dealkylation of tertiary amines.A large number of tertiary amines including some important synthetic drugs were N-dealkylated to give the corresponding secondary amines in 50-65percent yields.The reaction was carried out at room temperature by stirring a solution of a tertiary amine in methanol containing 10percent palladium-on-charcoal catalyst.The reaction had absolute requirement for molecular oxygen like the enzymatic dealkylation reaction.It also needed methanol to act as the reductant of molecular oxygen like the NADPH in the enzymatic reaction.A catalytic cycle similar to cytochrome P-450-catalysed oxygenation cycle is proposed for activation and transfer of oxygen to the α-carbon of tertiary amines to give unstable carbinolamines which on dissociation yield secondary amines.
