4741-62-2Relevant academic research and scientific papers
Palladium (II)-Catalyzed Decarboxylative Cross-Dehydrogenative Coupling: Direct Synthesis of meta-Substituted Biaryls from Aromatic Acids
Pu, Fan,Zhang, Lin-Yan,Liu, Zhong-Wen,Shi, Xian-Ying
supporting information, p. 2644 - 2649 (2018/07/29)
A palladium-catalyzed tandem process of simple aromatic acids has been achieved to afford meta-substituted biaryls in moderate to good yields. The reaction proceeds via carboxyl-directed intermolecular cross-dehydrogenative coupling and subsequent decarboxylation. The new C?C bonds in this transformation are formed in the ortho position of carboxyl and the reaction tolerates electron-rich acids. Both symmetrical and unsymmetrical meta-substituted biaryls can be directly synthesized via this method. (Figure presented.).
Synthesis, biological evaluation and molecular modeling studies of phthalazin-1(2: H)-one derivatives as novel cholinesterase inhibitors
Vila, Noemí,Besada, Pedro,Vi?a, Dolores,Sturlese, Mattia,Moro, Stefano,Terán, Carmen
, p. 46170 - 46185 (2016/06/09)
A new series of donepezil analogues based on the phthalazin-1(2H)-one scaffold was designed and synthesized with the aim of exploring its potential as human ChEIs. Biological results revealed that the structural modifications proposed significantly affected ChE inhibitory potency as well as selectivity for AChE/BuChE. Compound 1d showed promising in vitro inhibition of both enzymes in the μM range. However, most target compounds were significantly more active against AChE than BuChE, specifically 1f, 1h and 1j, with IC50 values in the low micromolar or submicromolar range, the most active compounds in the series. Docking simulations suggested that the most active compounds can recognize the donepezil binding site using a similar interactions network. These results allowed us to rationalize the observed structure-activity relationships. Moreover, the predicted physicochemical and ADME properties were also comparable to those of donepezil.
Synthesis, characterization and phytotoxic activity of hydroxylated isobenzofuran-1(3H)-ones
Teixeira,Pereira,Da Silva,Guilardi,Paix?o,Anconi,De Almeida,Ellena,Forlani
, p. 61 - 68 (2014/02/14)
Two hydroxylated isobenzofuranones 3 and 4 were synthesized from benzoic acids. The compounds were fully characterized by IR, NMR (1H and 13C), HRMS, and X-ray crystallography. Compounds 3 and 4 crystallized in the space group Pc and
Synthesis of Aromatic Esters, Lactones, Anhydrides, and Heterocycles via Thallation-Carbonylation of Arenes
Larock, Richard C.,Fellows, Constance A.
, p. 363 - 365 (2007/10/02)
The thallation and subsequent palladium-catalyzed carbonylation of simple arenes, benzylic and β-phenethyl alcohols, benzoic and phenylacetic acids, benzamide, and acetanilide afford benzoate esters, phthalides, 3,4-dihydroisocoumarins, phthalic and homophthalic anhydrides, phthalimide, and acetylanthranil, respectively.The carbonylation reaction proceeds in excellent yield at room temperature and atmospheric pressure and is highly stereo- and regioselective.
The Oxidation of a Series of Phthalyl Alcohols
Bhattacharjee, Debkumar,Popp, Frank D.
, p. 315 - 320 (2007/10/02)
A series of phthalyl alcohols containing methoxy and methyl substituents were prepared by lithium aluminum hydride reduction of phthalides.Oxidation of the phthalyl alcohols with activated manganese dioxide or with barium manganate gave phthalaldehydes or
