347977-58-6Relevant academic research and scientific papers
A concise formation of N-substituted 3,4-diarylpyrroles-synthesis and cytotoxic activity
Egorov, Maxim,Delpech, Bernard,Aubert, Genevieve,Cresteil, Thierry,Garcia-Alvarez, Maria Concepcion,Collin, Pascal,Marazano, Christian
supporting information, p. 1518 - 1524 (2014/03/21)
A short synthesis of N-substituted 3,4-diarylpyrroles by condensation of a phenacyl halide with a primary amine and a phenylacetaldehyde is reported. The key step is an intramolecular cyclization of an in situ generated enamine onto a ketone. Using differently substituted aromatic reactants and N-(3-aminopropyl)azatricyclodecane as the amine component, the preparation of analogs of the cytotoxic marine alkaloid halitulin could be achieved. The cytotoxicity of some of the compounds obtained by this method was studied, and one of them proved to be a very potent derivative, acting at a nanomolar concentration, in a caspase-independent cell death mechanism.
Synthesis and 2D QSAR of O-sulphonated β-aminols derivatives as novel antifungal and antibacterial agents
Saxena, Anil K.,Sharma, Sugandha,Pandey, Atindra K.,Shukla, Praveen K.
, p. 6476 - 6481 (2011/11/29)
Synthesis of a series of b-aminol derivatives using regioselective opening reaction catalyzed by SiO2 (60-120 mesh) and O-sulphonation in THF-KOH system, comprising tert-butoxycarbonyl at secondary nitrogen and evaluate for various stains of bacteria and fungi. SAR study of synthesized compound using backward regression analysis.
Synthesis of 4-substituted- and 1,4-disubstituted-4-hydroxypyrrolidin-2- ones
Kinsinger, Christopher R.,Tatko, Chad D.,Whelan, Christopher M.,Wilkinson, Timothy J.
, p. 1845 - 1852 (2008/02/02)
This report describes the synthesis of 4-substituted- and 1,4-disubstituted-4-hydroxypyrrolidin-2-ones by cyclization of intermediate γ-aminoesters prepared from alkylbenzylamines, α-bromoketones, and lithio ethyl acetate. Copyright Taylor & Francis Group, LLC.
Tetrahydroisoquinolines as subtype selective estrogen agonists/antagonists
Chesworth, Richard,Zawistoski, Michael P.,Lefker, Bruce A.,Cameron, Kimberly O.,Day, Robert F.,Mangano, F. Michael,Rosati, Robert L.,Colella, Stacy,Petersen, Donna N.,Brault, Amy,Lu, Bihong,Pan, Lydia C.,Perry, Pia,Ng, Oicheng,Castleberry, Tessa A.,Owen, Thomas A.,Brown, Thomas A.,Thompson, David D.,DaSilva-Jardine, Paul
, p. 2729 - 2733 (2007/10/03)
Two series of 6-hydroxy and 7-hydroxy tetrahydroisoquinolines were prepared. Evaluating a range of C-1, C-4, and N-substituents led to the discovery of ER α and ER β selective analogs.
Tetrahydroisoquinoline compounds as estrogen agonists/antagonists
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, (2008/06/13)
This invention relates to compounds useful for treating or preventing obesity, breast cancer, osteoporosis, endometriosis, cardiovascular disease, prostatic disease, and the like, and to pharmaceutical composition, methods, and kits comprising such compou
