94191-61-4Relevant academic research and scientific papers
HETEROARYL INHIBITORS OF PAD4
-
, (2018/03/28)
The present invention provides compounds useful as inhibitors of PAD4, compositions thereof, and methods of treating PAD4-related disorders.
Investigation of prototypal MOFs consisting of polyhedral cages with accessible Lewis-acid sites for quinoline synthesis
Gao, Wen-Yang,Leng, Kunyue,Cash, Lindsay,Chrzanowski, Matthew,Stackhouse, Chavis A.,Sun, Yinyong,Ma, Shengqian
supporting information, p. 4827 - 4829 (2015/03/18)
A series of prototypal metal-organic frameworks (MOFs) consisting of polyhedral cages with accessible Lewis-acid sites, have been systematically investigated for Friedl?nder annulation reaction, a straightforward approach to synthesizing quinoline and its derivatives. Amongst them MMCF-2 demonstrates significantly enhanced catalytic activity compared with the benchmark MOFs, HKUST-1 and MOF-505, as a result of a high-density of accessible Cu(II) Lewis acid sites and large window size in the cuboctahedral cage-based nanoreactor of MMCF-2.
Cu2+-doped zeolitic imidazolate frameworks (ZIF-8): Efficient and stable catalysts for cycloadditions and condensation reactions
Schejn, Aleksandra,Aboulaich, Abdelhay,Balan, Lavinia,Falk, Véronique,Lalevée, Jacques,Medjahdi, Ghouti,Aranda, Lionel,Mozet, Kevin,Schneider, Rapha?l
, p. 1829 - 1839 (2015/04/27)
Cu2+-doped zeolitic imidazolate framework (ZIF) crystals were efficiently prepared by reaction of Cu(NO3)2, Zn(NO3)2, and 2-methylimidazole in methanol at room temperature. Scanning electron microscopy, transmission electron microscopy and X-ray diffraction showed that the Cu/ZIF-8 particles were nanosized (between ca. 120 and 170 nm) and that the body-centered cubic crystal lattice of the parent ZIF-8 framework is continuously maintained, regardless of the doping percentage. Moreover, thermogravimetric analyses and specific BET surface area measurements demonstrated that the doping does not alter the high stability of ZIF-8 crystals and that the porosity only decreases at a high doping percentage (25% in Cu2+). The Cu/ZIF-8 material showed excellent catalytic activity in the [3 + 2] cycloaddition of organic azides with alkynes and in Friedl?nder and Combes condensations due to the high catalyst surface area and the high dispersion of Cu/ZIF-8 particles. Notably, the Cu/ZIF-8 particles not only exhibit excellent performance but also show great stability in the reaction, allowing their reuse up to ten times in condensation reactions. Our findings explored a simple and powerful way to incorporate metal ions into the backbones of open framework materials without losing their properties.
5 -CYANO-4, 6 -DIAMINOPYRIMIDINE OR 6 -AMINOPURINE DERIVATIVES AS PI3K- DELTA INHIBITORS
-
Page/Page column 60, (2012/05/20)
Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention aLso enables methods for treating cancers that are mediated, dependent on or associated with pi 105 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo- dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia ( T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.
The Reactions of Some ortho-Substituted Anilines With Various α,β-Acetylenic Ketones. A Route to Substituted Quinolines
Sinsky, M. S.,Bass, R. G.
, p. 759 - 768 (2007/10/02)
The reactions of some ortho-substituted anilines with various α,β-acetylenic ketones were investigated as a route to 4-alkyl-, 4-aryl-, 4-hydroxy-, and 4-amino-3-quinolyl ketones.The anilines examined were 2-aminoacetophenone (1), 2-aminobenzophenone (2), anthranilonitrile (3), methyl anthranilate (4), and ethyl anthranilate (5).The acetylenic ketones used were 1,4-diphenyl-2-butyne-1,4-dione (6), 3-butyn-2-one (7), 1,3-diphenyl-2-propyn-1-one (8), and 4-phenyl-3-butyn-2-one (9).The acetylenic ketones typically reacted with the anilines to give enamines; however, exceptions were found.Acetylene 6 reacts with 3 to give the enamine (13) along with a small amount of 2,3-dibenzoyl-4-quinolamine (14).The reactions of 1 or 2 with 6 give the respective quinoline derivatives directly.Acetylene 8 reacts with 2 to give 3-benzoyl-2,4-diphenylquinoline (22) directly, whereas no reaction occurs between 8 and 1 or 3.Acetylene 9 does not react with 1, 2 or 3.The enamines exist as the intramolecularly hydrogen bonded isomers and usually undergo cyclization with 5 molar equivalents of methanolic sodium methoxide to give quinoline derivatives.The 4-quinolinols exist predominantly as the 4-quinolinone tautomer.
