1687-68-9Relevant articles and documents
Identification of structural features of 2-alkylidene-1,3-dicarbonyl derivatives that induce inhibition and/or activation of histone acetyltransferases KAT3B/p300 and KAT2B/PCAF
Castellano, Sabrina,Milite, Ciro,Feoli, Alessandra,Viviano, Monica,Mai, Antonello,Novellino, Ettore,Tosco, Alessandra,Sbardella, Gianluca
, p. 144 - 157 (2015)
Dysregulation of the activity of lysine acetyltransferases (KATs) is related to a variety of diseases and/or pathological cellular states; however, their role remains unclear. Therefore, the development of selective modulators of these enzymes is of paramount importance, because these molecules could be invaluable tools for assessing the importance of KATs in several pathologies. We recently found that diethyl pentadecylidenemalonate (SPV106) possesses a previously unobserved inhibitor/activator activity profile against protein acetyltransferases. Herein, we report that manipulation of the carbonyl functions of a series of analogues of SPV106 yielded different activity profiles against KAT2B and KAT3B (pure KAT2B activator, pan-inhibitor, or mixed KAT2B activator/KAT3B inhibitor). Among the novel compounds, a few derivatives may be useful chemical tools for studying the mechanism of lysine acetylation and its implications in physiological and/or pathological processes.
Rational Optimization of Lewis-Acid Catalysts for Direct Alcohol Amination, Part 2 – Titanium Triflimide as New Active Catalyst
Payard, Pierre-Adrien,Finidori, Céline,Guichard, Laurélia,Cartigny, Damien,Corbet, Matthieu,Khrouz, Lhoussain,Bonneviot, Laurent,Wischert, Raphael,Grimaud, Laurence,Pera-Titus, Marc
supporting information, p. 3225 - 3228 (2020/06/08)
The reactivity of a new titanium triflimide salt (see Part 1) was investigated for the direct amination of alcohols. The combination of this new Lewis acid with pyridine-based ligands allowed a significant increase of activity. The scope of the reaction was increased compared to other Lewis-acid-based protocols. Finally, mechanistic insights based on EPR spectroscopy and DFT calculations are provided.
Manganese catalyzed reductive amination of aldehydes using hydrogen as a reductant
Wei, Duo,Bruneau-Voisine, Antoine,Valyaev, Dmitry A.,Lugan, No?l,Sortais, Jean-Baptiste
, p. 4302 - 4305 (2018/05/03)
A one-pot two-step procedure was developed for the alkylation of amines via reductive amination of aldehydes using molecular dihydrogen as a reductant in the presence of a manganese pyridinyl-phosphine complex as a pre-catalyst. After the initial condensation step, the reduction of imines formed in situ is performed under mild conditions (50-100 °C) with 2 mol% of catalyst and 5 mol% of tBuOK under 50 bar of hydrogen. Excellent yields (>90%) were obtained for a large combination of aldehydes and amines (40 examples), including aliphatic aldehydes and amino-alcohols.