6328-48-9Relevant articles and documents
QUINAZOLINE DERIVATIVES AS TYROSINE KINASE INHIBITOR, COMPOSITIONS, METHODS OF MAKING THEM AND THEIR USE
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Page/Page column 497, (2020/05/13)
The present disclosure relates to new compounds or pharmaceutically acceptable salts or stereoisomers thereof of formula I as inhibitors of receptor tyrosine kinases (RTK), in particular extracellular mutants of ErbB-receptors. The present disclosure also relates to methods of preparation these compounds, compositions comprising these compounds, and methods of using them in the treatment of cancer in mammals (e.g. humans).
Formation of a New, Strongly Basic Nitrogen Anion by Metal Oxide Modification
Tamura, Masazumi,Kishi, Ryota,Nakayama, Akira,Nakagawa, Yoshinao,Hasegawa, Jun-Ya,Tomishige, Keiichi
, p. 11857 - 11867 (2017/09/08)
Development of new hybrid materials having unique and unprecedented catalytic properties is a challenge for chemists, and heterogeneous-homogeneous hybrid catalysts have attracted much attention because of the preferable and exceptional properties that are highly expected to result from combination of the components. Base catalysts are widely used in organic synthesis as key materials, and a new class of base catalysts has made a large impact from academic and industrial viewpoints. Here, a principle for creating a new strong base by hybridization of homogeneous and heterogeneous components is presented. It is based on the modification of organic compounds with metal oxides by using the acid-base property of metal oxides. Based on kinetic and DFT studies, combination of CeO2 and 2-cyanopyridine drastically enhanced the basicity of 2-cyanopyridine by a factor of about 109 (～9 by pKa (in CH3CN)), and the pKa was estimated to be ～21, which locates it in the superbase category. 2-Cyanopyridine and CeO2 formed a unique adsorption complex via two interaction modes: (i) coordinative interaction between the Ce atom of CeO2 and the N atom of the pyridine ring in 2-cyanopyridine, and (ii) covalent interaction between the surface O atom of CeO2 and the C atom of the CN group in 2-cyanopyridine by addition of the lattice oxygen of CeO2 to the CN group of 2-cyanopyridine. These interactions established a new, strongly basic site of N- over the CeO2 surface.
Organocatalytic conjugate addition of cyclopropylacetaldehyde derivatives to nitro olefins: En route to β- and γ-amino acids
Kaasik, Mikk,Noole, Artur,Reitel, K?rt,J?rving, Ivar,Kanger, T?nis
, p. 1745 - 1753 (2015/05/27)
Cyclopropane-containing amino acids are important pharmaceuticals and biologically active compounds. A new organocatalytic asymmetric Michael reaction has been developed. This allows the one-step introduction of the cyclopropane ring, as well as two different nitrogen-containing functional groups (tert-butoxycarbonylamino and nitro) into the target compounds. All the products were isolated in good yields with moderate to excellent enantio- and diastereoselectivities.
