50458-78-1Relevant articles and documents
Microscale Parallel Synthesis of Acylated Aminotriazoles Enabling the Development of Factor XIIa and Thrombin Inhibitors
Platte, Simon,Korff, Marvin,Imberg, Lukas,Balicioglu, Ilker,Erbacher, Catharina,Will, Jonas M.,Daniliuc, Constantin G.,Karst, Uwe,Kalinin, Dmitrii V.
supporting information, p. 3672 - 3690 (2021/08/07)
Herein we report a microscale parallel synthetic approach allowing for rapid access to libraries of N-acylated aminotriazoles and screening of their inhibitory activity against factor XIIa (FXIIa) and thrombin, which are targets for antithrombotic drugs. This approach, in combination with post-screening structure optimization, yielded a potent 7 nM inhibitor of FXIIa and a 25 nM thrombin inhibitor; both compounds showed no inhibition of the other tested serine proteases. Selected N-acylated aminotriazoles exhibited anticoagulant properties in vitro influencing the intrinsic blood coagulation pathway, but not extrinsic coagulation. Mechanistic studies of FXIIa inhibition suggested that synthesized N-acylated aminotriazoles are covalent inhibitors of FXIIa. These synthesized compounds may serve as a promising starting point for the development of novel antithrombotic drugs.
Pd-containing organopolyoxometalates derived from Dawson polyoxometalate [P2W15V3O62]9-: Lewis acidity and dual site catalysis
Riflade, Benoit,Lachkar, David,Oble, Julie,Li, Joaquim,Thorimbert, Serge,Hasenknopf, Bernold,Lacote, Emmanuel
supporting information, p. 3860 - 3863 (2014/08/18)
Grafting of a palladium complex to the Dawson vanadotungstate polyanion [P2W15V3O62]9- via an organic ligand generates a large family of pincer-type hybrid polyoxometalates. The palladium-POM derivatives have dual catalytic properties. Unlike their parent inorganic polyanions, they catalyze allylations while retaining their oxidant character, which leads to single-pot dual site catalysis. This opens a new route for multicatalytic reactions.
A novel synthesis of isoquinolines containing an electron withdrawing substituent
Kohno, Harumichi,Yamada, Koichiro
, p. 103 - 117 (2007/10/03)
3,4-Dihydroisoquinolines (10, 13) and isoquinolines (11), having various electron withdrawing substituent were synthesized in two steps from N- benzenesulfonyl- or N, N-dimethylsulfamoyl-β-phenethylamines (2 and 5). A novel cyclization method using ethyl chloro(methylthio)acetate (1) in the presence of SnCl4 as Lewis acid, followed by acid or base treatment provides the title compounds in good yield.