23826-72-4Relevant articles and documents
C2 amination of pyridine with primary amines mediated by sodium hydride in the presence of lithium iodide
Chiba, Shunsuke,Ong, Derek Yiren,Pang, Jia Hao
, p. 363 - 373 (2021/11/16)
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Design, synthesis and biological activity of a novel ethylenediamine derivatives as H1 receptor antagonists
Chen, Guangying,Huang, Gangliang,Zhou, Shiyang
, (2019/11/21)
In this study, a series of novel ethylenediamine compounds were obtained by structural modification of the lead compounds with thonzylamine, and using the principle of modifying by bioisostere formation and modification with alkyl groups. In vitro assay, the biological activities showed that the target compounds have good properties in inhibiting mast cell degranulation and releasing histamine and β-aminohexidase, such as the compounds 5c, 5g, 5k, 5l and 5o, especially of compound 5k to mast cell degranulation is IC50 = 0.0106 ± 0.001 μmol?L?1, histamine release was IC50 = 0.0192 ± 0.005 μmol?L?1 and β-hexosaminidase release was IC50 = 0.0455 ± 0.002 μmol?L?1 in vitro. At the same time, in vivo biological activities assay results showed that have a good Histamie induce bronchospasm effect with relatively long duration and good protective effect in vivo, among which the protective effect of compound 5k was 79.74 ± 0.30%, compounds 5c, 5g, 5k, 5l and 5o could inhibit the capillary permeability of increasing which were caused by histamine.
Reinvestigating Raney nickel mediated selective alkylation of amines with alcohols via hydrogen autotransfer methodology
Mehta, Astha,Thaker,Londhe,Nandan, Santosh R.
, p. 241 - 251 (2014/05/20)
An efficient, cost-effective use of Raney nickel (R-Ni) a widely used industrial catalyst for N-alkylation using alcohols is highlighted here. The work describes the scope and capability of R-Ni in hydrogen autotransfer reactions enabling its widespread use in the Chemical and Pharmaceutical industry. R-Ni of W4, T4, and W7 grades were prepared and evaluated for alkylation of amines. The best activity and selectivity for mono alkylation of amines were obtained using W4 R-Ni at 1:4 moles of amine to alcohol in xylene at reflux. T4 R-Ni also showed ability to form stable imines. The prepared R-Ni was also recycled and reused for N-alkylation reaction. The optimized methodology was applied for synthesis of Active Pharmaceutical ingredients Piribedil and Mepyramine. The simplicity and wide substrate scope makes this method a preferred Hydrogen Auto-transfer protocol for the alkylation of amines.
