14025-83-3Relevant academic research and scientific papers
Enantioselective Copper-Catalyzed Radical Ring-Opening Cyanation of Cyclopropanols and Cyclopropanone Acetals
Chen, Pinghong,Guo, Yin-Long,Liu, Guosheng,Wang, Lei,Wu, Lianqian
supporting information, p. 2189 - 2194 (2020/04/17)
A novel approach for enantioselective cyanation of cyclopropanols and their derivatives through copper-catalyzed radical relay processes has been developed. Various cyclopropanols and cyclopropanone acetals are compatible to the catalytic conditions, providing β-carbonyl nitriles with excellent enantioselectivity. These products can be readily converted to chiral γ-amino acids derivatives and drugs such as (R)-baclofen. Preliminary mechanistic studies have supported a ring-opening process for cyclopropanoxy radicals followed by copper-catalyzed enantioselective cyanation of benzylic radicals to form the C?CN bonds in an enantioselective manner. (Figure presented.).
Nano-K2CO3: Preparation, characterization and evaluation of reactive activities
Li, Jun-Zhang,Fan, Shi-Ming,Sun, Xuan-Fei,Liu, Shouxin
, p. 1865 - 1869 (2016/01/20)
A novel base, nano-K2CO3, was easily prepared by ultrafine wet milling. The surface properties and the reactive activities of nano-K2CO3 were characterized. It was found that such a base showed higher basicity than normal K2CO3 and could replace sodium (or potassium) alkoxide to carry out monoalkylation and oximation of active methylene compounds. The nano-K2CO3 could be regenarated and reused 10 times without loss of its reactive activity.
DERIVATIVES OF 2-PYRIDIN-2-YL-PYRAZOL-3(2H)-ONE, PREPARATION AND THERAPEUTIC USE THEREOF AS HIF ACTIVATORS
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Page/Page column 26, (2011/12/13)
The present invention relates to novel substituted dihydropyrazolone derivatives, to their preparation and to their therapeutic use as activators of the transcription factor HIF.
Synthesis and evaluation of 2-phenyl-1,4-butanediamine-based CCR5 antagonists for the treatment of HIV-1
Tallant, Matthew D.,Duan, Maosheng,Freeman, George A.,Ferris, Robert G.,Edelstein, Mark P.,Kazmierski, Wieslaw M.,Wheelan, Pat J.
scheme or table, p. 1394 - 1398 (2011/04/16)
We describe the synthesis and potency of a novel series of N-substituted 2-phenyl- and 2-methyl-2-phenyl-1,4-diaminobutane- based CCR5 antagonists. Compounds 7a and 12f were found to be potent in anti-HIV assays and bioavailable in the low-dose rat PK model.
THERAPEUTIC COMPOUNDS
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Page/Page column 17, (2011/02/24)
The present invention relates to compounds of Formula (I) and (Ia) useful in the treatment of CCR5-related diseases and disorders, for example, the prevention or treatment of an HIV infection, and in the treatment of the resulting acquired immune deficien
TETRAHYDRO ISOQUINOLINE DERIVATIVES, PREPARATION METHODS AND MEDICINAL USES THEREOF
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Page/Page column 8, (2009/04/23)
A kind of tetrahydro isoquinoline derivatives (I), their preparation methods, medicine compositions and medicinal uses thereof, especially their uses as κ-opioid receptor excitant in pain relieving, which belongs to the medicine chemistry. The substituents R1, R2, R3, R4 of general formula (I) are defined as the description.
Synthesis of 3,3-and 4,4-alkyl-phenyl-substituted pyrrolidin-2-one derivatives
Kulig,Ignasik,Malawska
experimental part, p. 1629 - 1636 (2010/07/06)
Syntheses of 3,3-and 4,4-alkyl-phenyl-substituted pyrrolidin-2-one derivatives are described. The final compounds were obtained by the reductive cyclization of relevant cyanoalkanoate esters using NaBH4 and CoCl2.6H2O. The obtained pyrroIidin-2-one derivatives are pharmacophoric fragments for the synthesis of various biologically active compounds.
Tetrahydro isoquinoline derivatives, preparation methods and medicinal uses thereof
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Page/Page column 6, (2009/12/02)
A kind of tetrahydro isoquinoline derivatives (I), their preparation methods, medicine compositions and medicinal uses thereof, especially their uses as kappa-opioid receptor excitant in pain relieving, which belongs to the medicine chemistry. The substituents R1, R2, R3, R4 of general formula (I) are defined as the description.
A convenient synthesis of 3-arylbutanolides and 3-arylbutenolides
Gu, Jian-Xin,Holland, Herbert L.
, p. 3305 - 3315 (2007/10/03)
A series of 3-aryl-substituted butenolides and butanolides has been prepared in a common short synthetic sequence from the corresponding aryl aldehydes. The 3-arylbutanolides are prepared by cyclisation of 3-aryl-3- cyano-1-propanols, obtained by selectiv
