13298-49-2Relevant academic research and scientific papers
I2-Promoted [3+2] Cyclization of 1,3-Diketones with Potassium Thiocyanate: a Route to Thiazol-2(3H)-One Derivatives
An, Zhenyu,Liu, Yafeng,Yan, Rulong,Zhao, Pengbo
supporting information, p. 3240 - 3244 (2021/06/16)
An I2-promoted strategy has been developed for the synthesis of thiazol-2(3H)-one derivatives from 1,3-diketones with potassium thiocyanate. This [3+2] cyclization reaction involves C?S and C?N bond formation and exhibits good functional group tolerance. A series of thiazol-2(3H)-one derivatives are obtained in moderate to good yields. (Figure presented.).
A General Proline-Catalyzed Synthesis of 4,5-Disubstituted N-Sulfonyl-1,2,3-Triazoles from 1,3-Dicarbonyl Compounds and Sulfonyl Azide
Rajasekar, Shanmugam,Anbarasan, Pazhamalai
supporting information, p. 4563 - 4567 (2019/11/03)
An efficient proline-catalyzed synthesis of 4,5-disubstituted-N-sulfonyl-1,2,3-triazoles has been accomplished from 1,3-dicarbonyl compounds and sulfonyl azides. The developed reaction is suitable for various symmetrical and unsymmetrical 1,3-dicarbonyl compounds, tolerates various functional groups and affords 4,5-disubstituted-N-sulfonyl-1,2,3-triazoles in good yield with excellent regioselectivity. Rhodium-catalyzed denitrogenative functionalization of 4,5-disubstituted-N-sulfonyl-1,2,3-triazoles further demonstrates their utility in organic synthesis.
Design, synthesis, and evaluation of multitarget-directed ligands against Alzheimer's disease based on the fusion of donepezil and curcumin
Yan, Jun,Hu, Jinhui,Liu, Anqiu,He, Lin,Li, Xingshu,Wei, Hui
, p. 2946 - 2955 (2017/05/25)
By fusing donepezil and curcumin, a novel series of compounds were obtained as multitarget-directed ligands against Alzheimer's disease. Among them, compound 11b displayed potent acetylcholinesterase (AChE) inhibition (IC50?=?187?nM) and the highest BuChE/AChE selectivity (66.3). Compound 11b also inhibited 45.3% Aβ1–42 self-aggregation at 20?μM and displayed remarkable antioxidant effects. The metal-chelating property of compound 11b was elucidated by determining the 1:1 stoichiometry for the 11b–Cu(II) complex. The excellent blood–brain barrier permeability of 11b also indicated the potential for the compound to penetrate the central nervous system.
Direct route to 1,3-diketones by palladium-catalyzed carbonylative coupling of aryl halides with acetylacetone
Korsager, Signe,Nielsen, Dennis U.,Taaning, Rolf H.,Lindhardt, Anders T.,Skrydstrup, Troels
supporting information, p. 17687 - 17691 (2014/01/17)
Man up your magnesium! By employing a MgCl2/Et3N system, aryl diketones can be generated from the Pd-catalyzed carbonylative α-arylation of acetylacetone with aryl bromides (see scheme). The method is ideal for the introduction of carbon isotopes into more complex structures, since only stoichiometric amounts of carbon monoxide are employed. Copyright
Pyrazoloisoquinoline derivative as kinase inhibitors for the treatment of various disorders
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Page 15, (2010/02/10)
Compounds of the formula I are suitable for producing pharmaceuticals for the prophylaxis and therapy of diseases whose course involves an increased activity of NIK.
PYRAZOLOISOQUINOLINE DERIVATIVES AS KINASE INHIBITORS
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Page/Page column 34-35, (2010/02/10)
Novel pyrazoloisoquinoline derivatives as kinase inhibitors are disclosed which are suitable for producing pharmaceuticals for the prophylaxis and therapy of diseases whose course involves an increased activity of NIK.
PYRAZOLOISOQUINOLINE DERIVATIVES FOR INHIBITING NFKAPPAB-INDUCING KINASE (NIK)
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Page/Page column 22, (2008/06/13)
The invention relates to compounds of formula (I), which are suitable for producing medicaments for the prophylaxis and treatment of diseases, the progression of which involves an increased activity of NIK.
