117155-90-5Relevant academic research and scientific papers
Synthesis, biological activity and in silico pharmacokinetic prediction of a new 2-thioxo-imidazoldidin-4-one of primaquine
Pereira, Mariana,Caljon, Guy,Gouveia, Maria Jo?o,Maes, Louis,Vale, Nuno
, p. 1 - 11 (2021)
The discovery of novel antiparasitic drugs for neglected tropical diseases (NTDs) constitutes a global urgency and requires a range of innovative strategies to ensure a sustainable pipeline of lead compounds. Thus far, primaquine (PQ) is the only transmis
Iodoacetic acid is an efficient reagent for the synthesis of amino acid derived 2-aminobenzimidazoles
Krasikovs, Andrejs,Ozola, Vita,Dax, Scott L.,Suna, Edgars
, p. 683 - 693 (2013/04/10)
Chiral, nonracemic, N-unprotected amino acids were converted into the corresponding N-benzimidazol-2-yl derivatives by a sequential procedure involving initial formation of isothiocyanates, their reaction with arene-1,2-diamines, and cyclization-desulfurization of the intermediate thioureas with iodoacetic acid. The simplified workup and the lack of volatile or toxic byproducts in the key desulfurization step renders iodoacetic acid a superior reagent to the usual reagent, iodomethane. Georg Thieme Verlag Stuttgart · New York.
Enantioselective aza-Michael addition of imides by using an integrated strategy involving the synthesis of a family of multifunctional catalysts, usage of multiple catalysis, and rational design of experiment
Silvi, Mattia,Renzi, Polyssena,Rosato, Deborah,Margarita, Cristiana,Vecchioni, Alessio,Bordacchini, Ivan,Morra, Diego,Nicolosi, Alessandro,Cari, Riccardo,Sciubba, Fabio,Scarpino Schietroma, Daniele M.,Bella, Marco
supporting information, p. 9973 - 9978 (2013/08/23)
A challenging asymmetric reaction (aza-Michael addition of imides to enones) has been optimized through an integrated approach involving the synthesis of a family of organocatalysts, multiple catalysis (usage of additives), and finally with rational explo
Primary amine-thioureas based on tert-butyl esters of natural amino acids as organocatalysts for the Michael reaction
Kokotos, Christoforos G.,Kokotos, George
experimental part, p. 1355 - 1362 (2009/12/09)
A new class of primary amine-thioureas based on tert-butyl esters of (S)-α-amino acids and (1S,2S)-diphenylethylenediamine was synthesized and their activity as catalysts in Michael additions was evaluated. Derivatives based on di-tert-butyl aspartate and
A new efficient synthesis of isothiocyanates from amines using di-tert-butyl dicarbonate
Munch, Henrik,Hansen, Jon S.,Pittelkow, Michael,Christensen, J?rn B.,Boas, Ulrik
, p. 3117 - 3119 (2008/09/20)
Alkyl and aryl amines are converted smoothly to the corresponding isothiocyanates via the dithiocarbamates in good to excellent yields using di-tert-butyl dicarbonate (Boc2O) and 1-3 mol % of DMAP or DABCO as catalyst. As most of the byproducts are volatile, the work-up involves simple evaporation of the reaction mixture.
Synthesis and solution thermodynamic study of rigidified and functionalised EGTA derivatives
Tei, Lorenzo,Baranyai, Zsolt,Botta, Mauro,Piscopo, Laura,Aime, Silvio,Giovenzana, Giovanni B.
experimental part, p. 2361 - 2368 (2009/02/02)
The synthesis of a new series of EGTA (ethyleneglycol-bis(2- aminoethylether)-N,N,N′,N′-tetraacetic acid) derivatives incorporating aromatic and functionalized aromatic moieties into the oxoethylenic bridge is described. A solution thermodynamic study was
Maximizing the relaxivity of HSA-bound gadolinium complexes by simultaneous optimization of rotation and water exchange
Avedano, Stefano,Tei, Lorenzo,Lombardi, Alberto,Giovenzana, Giovanni B.,Aime, Silvio,Longo, Dario,Botta, Mauro
, p. 4726 - 4728 (2008/09/16)
Two new GdEGTA (EGTA = ethylene glycol-bis(2-aminoethylether)-N,N,N′, N′-tetraacetic acid) derivatives incorporating aromatic moieties into the oxoethylenic bridge have been prepared and characterised, their conjugates to HSA investigated and an unprecede
