68104-61-0Relevant academic research and scientific papers
(DiMeIHeptCl)Pd: A Low-Load Catalyst for Solvent-Free (Melt) Amination
Semeniuchenko, Volodymyr,Sharif, Sepideh,Day, Jonathan,Chandrasoma, Nalin,Pietro, William J.,Manthorpe, Jeffrey,Braje, Wilfried M.,Organ, Michael G.
, p. 10343 - 10359 (2021/07/31)
(DiMeIHeptCl)Pd, a hyper-branched N-aryl Pd NHC catalyst, has been shown to be efficient at performing amine arylation reactions in solvent-free ("melt") conditions. The highly lipophilic environment of the alkyl chains flanking the Pd center serves as lubricant to allow the complex to navigate through the paste-like environment of these mixtures. The protocol can be used on a multi-gram scale to make a variety of aniline derivatives, including substrates containing alcohol moieties.
MACROCYCLIC BROAD SPECTRUM ANTIBIOTICS
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Paragraph 00806; 00807, (2018/09/12)
Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.
NOVEL 1,6-DISUBSTITUTED-3-AMINO-4,5,6,7-TETRAHYDRO-1H-PYRAZOLO[3,4-C]PYRIDIN-7-ONE COMPOUNDS AND PREPARATION THEREOF
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Page/Page column 6, (2012/01/13)
Provided are a novel 1,6-disubstituted-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-7-one compound, a pharmaceutically acceptable salt compound thereof, a method for preparing the compound, and an anticancer pharmaceutical composition including the compound as an effective ingredient.
New pyrimido[5,4-b]indoles as ligands for α1-adrenoceptor subtypes
Romeo, Giuseppe,Materia, Luisa,Manetti, Fabrizio,Cagnotto, Alfredo,Mennini, Tiziana,Nicoletti, Ferdinando,Botta, Maurizio,Russo, Filippo,Minneman, Kenneth P.
, p. 2877 - 2894 (2007/10/03)
A new series of compounds were designed as structural analogues of the α1-AR ligand RN5 (4), characterized by a tricyclic 5H-pyrimido[5,4-b]indole-(1H,3H)2,4-dione system connected through an alkyl chain to a phenylpiperazine (PP) moiety. These compounds were synthesized and tested in binding assays on human α1A-AR, α1B-AR, and α1D-AR subtypes expressed in HEK293 cells. Several structural modifications were performed on the PP moiety, the tricyclic system, and the connecting alkyl chain. Many of the new molecules showed a preferential affinity for the α1D-AR subtype. Some compounds, including 39 and 40, displayed substantial α1D-AR selectivity with respect to α1A-AR, α1B-AR, serotonergic 5-HT1A, 5-HT1B, 5-HT2A, and dopaminergic D1 and D2 receptors. Two conformationally rigid analogues of 4, useful for studying the architecture of the receptor/ligand complex, were also prepared and tested. A subset of the new compounds was then used to evolve a preliminary pharmacophore model for α1D-AR antagonists, based on a more generalized model we had developed for α1-AR antagonists. This new model rationalized the relationships between structural properties and biological data of the pyrimido[5,4-b]indole compounds, as well as other compounds.
