28163-67-9Relevant academic research and scientific papers
Quinazoline derivatives and its preparation method and application
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Paragraph 0041-0045; 0086-0089, (2019/07/08)
The invention relates to quinazoline derivatives and its preparation method and application. The quinazoline derivatives with The structural formula, the quinazoline derivative to gefitinib for the positive control, the result shows that compared with the gefitinib has good activity; and lead compound OTS514 compared, equivalent activity, PBK/TOPK inhibitors for further transformation and the discovery of new anti-tumor medicine phenological shopping has higher learning with the reference value. The invention also provides a preparation method of the quinazoline derivatives and the preparation of PBK/TOPK inhibitor and an anticancer drug.
Rhodium-catalyzed asymmetric hydrogenation of β-branched enamides for the synthesis of β-stereogenic amines
Zhang, Jian,Liu, Chong,Wang, Xingguang,Chen, Jianzhong,Zhang, Zhenfeng,Zhang, Wanbin
, p. 6024 - 6027 (2018/06/18)
Using a rhodium complex of a bisphosphine ligand (R)-SDP, β-branched simple enamides with a (Z)-configuration were hydrogenated to β-stereogenic amines in quantitative yields and with excellent enantioselectivities (88-96% ee).
Novel chiral phosphine ligand, metal catalyst containing chiral phosphine ligand and preparation method and application thereof
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Paragraph 0075; 0076, (2016/11/21)
The invention provides a novel chiral phosphine ligand, a metal catalyst containing the chiral phosphine ligand and a preparation method and an application thereof. The novel chiral phosphine ligand has a structural formula shown in the attached figure; the metal catalyst is a transition metal complex which is synthesized by the novel chiral phosphine ligand and transition metal, and is used for asymmetric catalyzing and hydrogenating reaction, and catalyzing and hydrogenating to synthesize beta-arylamide with high optical purity. The novel chiral phosphine ligand has the advantages that the economic practicality is higher, the product purity is high, the carrying amount of ligand (S/C) is high, and the like.
New insight into the role of a base in the mechanism of imine transfer hydrogenation on a Ru(ii) half-sandwich complex
Kuzma, Marek,Václavík, Ji?í,Novák, Petr,P?ech, Jan,Janu??ák, Jakub,?erveny, Jaroslav,Pechá?ek, Jan,?ot, Petr,Vilhanová, Beáta,Matou?ek, Václav,Goncharova, Iryna I.,Urbanová, Marie,Ka?er, Petr
, p. 5174 - 5182 (2013/04/23)
Asymmetric transfer hydrogenation (ATH) of cyclic imines using [RuCl(η6-p-cymene)TsDPEN] (TsDPEN = N-tosyl-1,2- diphenylethylenediamine) was tested with various aliphatic (secondary, tertiary) and aromatic amines employed in the HCOOH-base hydrogen donor mixture. Significant differences in reaction rates and stereoselectivity were observed, which pointed to the fact that the role of the base in the overall mechanism could be more significant than generally accepted. The hydrogenation mixture was studied by nuclear magnetic resonance (NMR), Fourier transform ion cyclotron resonance mass spectrometry (FT-ICR MS) and vibrational circular dichroism (VCD) with infrared spectroscopy. The results suggested that the protonated base formed an associate with the active ruthenium-hydride species, most probably via a hydrogen bond with the sulfonyl group of the complex. It is assumed that the steric and electronic differences among the bases were responsible for the results of the initial ATH experiments.
Asymmetric hydrogenation of protected allylic amines
Steinhuebel, Dietrich P.,Krska, Shane W.,Alorati, Anthony,Baxter, Jenny M.,Belyk, Kevin,Bishop, Brian,Palucki, Michael,Sun, Yongkui,Davies, Ian W.
supporting information; experimental part, p. 4201 - 4203 (2010/11/19)
A general method for the enantioselective hydrogenation of protected allylic amine derivatives is described. This procedure relies on the generation of a cationic ruthenium complex with the axially chiral ligand (-)-TMBTP. The utility is highlighted by th
