79205-36-0Relevant academic research and scientific papers
An Easy-to-Machine Electrochemical Flow Microreactor: Efficient Synthesis of Isoindolinone and Flow Functionalization
Folgueiras-Amador, Ana A.,Philipps, Kai,Guilbaud, Sébastien,Poelakker, Jarno,Wirth, Thomas
supporting information, p. 15446 - 15450 (2017/11/10)
Flow electrochemistry is an efficient methodology to generate radical intermediates. An electrochemical flow microreactor has been designed and manufactured to improve the efficiency of electrochemical flow reactions. With this device only little or no supporting electrolytes are needed, making processes less costly and enabling easier purification. This is demonstrated by the facile synthesis of amidyl radicals used in intramolecular hydroaminations to produce isoindolinones. The combination with inline mass spectrometry facilitates a much easier combination of chemical steps in a single flow process.
Selenium-mediated synthesis of biaryls through rearrangement
Shahzad, Sohail A.,Vivant, Clotilde,Wirth, Thomas
supporting information; experimental part, p. 1364 - 1367 (2010/06/17)
"Chemical Equation Presented" A new cyclization of β-keto ester substituted stilbene derivatives using selenium electrophiles in the presence of Lewis acids is described. Substituted naphthols are obtained through cyclization and subsequent 1,2-rearrangement of aryl groups under very mild reaction conditions.
Diselenide- and disulfide-mediated synthesis of isocoumarins
Shahzad, Sohail A.,Venin, Claire,Wirth, Thomas
experimental part, p. 3465 - 3472 (2010/09/07)
Cyclizations of stilbenecarboxylic acids to the corresponding isocoumarin derivatives using diselenide or disulfide reagents have been developed. By employing bis(triflouroacetoxy)iodobenzene as oxidant for the 6-endo-trig cyclizations a variety of dihydroisocoumarins have been prepared in good yields. This method is capable of forming isocoumarins and dihydroisocoumarin derivatives by a cyclization-elimination route.
Benzoylalanine-derived ketoamides carrying vinylbenzyl amino residues: Discovery of potent water-soluble calpain inhibitors with oral bioavailability
Lubisch, Wilfried,Beckenbach, Edith,Bopp, Sabina,Hofmann, Hans-Peter,Kartal, Arzu,K?stel, Claudia,Lindner, Tanja,Metz-Garrecht, Marion,Reeb, Jutta,Regner, Ferdinand,Vierling, Michael,M?ller, Achim
, p. 2404 - 2412 (2007/10/03)
Novel benzoylalanine-derived ketoamides were prepared and evaluated for calpain I inhibition. Derivatives carrying vinylbenzyl amino residues in the P2 - P3 region inhibited calpain in nanomolar concentrations and thus represent a novel class of nonpeptidic calpain inhibitors. Selected examples exhibited an improved pharmacokinetic profile including improved watersolubility and metabolic stability. In particular, these calpain inhibitors showed oral bioavailability in rats as demonstrated by N-(1-benzyl-2-carbamoyl-2-oxoethyl)-2- [E-2-(4-diethylaminomethylphenyl)ethen-1-yl]benzamide (5d). The closely related derivative N-(1-carbamoyl-1-oxohex-1-yl)-2-[E-2- (4-dimethylaminomethylphenyl)-ethen-1-yl]benzamide (5b) was evaluated for neuroprotective efficacy after experimental traumatic brain injury in a fluid percussion model in rats. When administered after injury, 5b reduced the number of damaged neurons by 41%, and this result would be in line with the suggested neuroprotective efficacy of calpain inhibition.
Benzamidoaldehydes and their use as cysteine protease inhibitors
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, (2008/06/13)
Compounds of the formula where R1, R2, R3, X and n are as defined in the description, are inhibitors of cysteine protease.
Ketobenzamides as calpain inhibitors
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, (2008/06/13)
PCT No. PCT/EP97/06655 Sec. 371 Date Jun. 8, 1999 Sec. 102(e) Date Jun. 8, 1999 PCT Filed Nov. 28, 1997 PCT Pub. No. WO98/25883 PCT Pub. Date Jun. 18, 1998The patent describes ketobenzamides of the formula where R1, R2, R3, R4, X and n have the meanings g
The Synthesis and Anti-geotropic Activity of o-Arylethenylbenzoic Acids
Teitei, Tsutomu
, p. 1669 - 1674 (2007/10/02)
Fourteen new and three known o-arylethenylbenzoic acids (10-18), required for testing as potential plant growth regulators, have been synthesized by the Wittig reaction.The cis- and trans-isomers were separated by fractional crystallization and identified by NMR spectroscopy.The preliminary assay results on cress seedlings are reported and show that both geometric isomers appear to have nearly identical anti-geotropic activity in this test system.
