582-22-9Relevant articles and documents
CO2-Assisted asymmetric hydrogenation of prochiral allylamines
Alridge, Christopher J.,De Winter, Tamara M.,Ho, Jaddie,Jessop, Philip G.
, p. 6755 - 6761 (2022/03/31)
A new methodology for the asymmetric hydrogenation of allylamines takes advantage of a reversible reaction between amines and carbon dioxide (CO2) to suppress unwanted side reactions. The effects of various parameters (pressure, time, solvent, and base additives) on the enantioselectivity and conversion of the reaction were studied. The homogeneously-catalyzed asymmetric hydrogenation of 2-arylprop- 2-en-1-amine resulted in complete conversion and up to 82% enantiomeric excess (ee). Added base, if chosen carefully, improves the enantioselectivity and chemoselectivity of the overall reaction.
Iron-Catalyzed Diastereoselective Synthesis of Disubstituted Morpholines via C-O or C-N Bond Formation
Aubineau, Thomas,Dupas, Alexandre,Zeng, Tian,Cossy, Janine
supporting information, p. 525 - 531 (2020/08/28)
The diastereoselective synthesis of 2,6- and 3,5-disubstituted morpholines was achieved from 1,2-amino ethers and 1,2-hydroxy amines substituted by an allylic alcohol using an iron(III) catalyst. The morpholines were obtained either by C-O or C-N bond formation. A plausible mechanism is suggested, involving a thermodynamic equilibrium to explain the formation of the cis diastereoisomer as the major product.
Quinazoline derivatives and its preparation method and application
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Paragraph 0041-0045, (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.