136832-46-7Relevant academic research and scientific papers
Novel 5-cyclopropyl-1,4-benzodiazepin-2-ones as potent and selective IKs-blocking class III antiarrhythmic agents
Butcher, John W.,Liverton, Nigel J.,Claremon, David A.,Freidinger, Roger M.,Jurkiewicz, Nancy K.,Lynch, Joseph J.,Salata, Joseph J.,Wang, Jixin,Dieckhaus, Christine M.,Slaughter, Donald E.,Vyas, Kamlesh
, p. 1165 - 1168 (2003)
Novel 5-cyclopropyl-1,4-benzodiazepin-2-ones having various N-l substituents were identified as potent and selective blockers of the slowly activating cardiac delayed rectifier potassium current (IKs). Compound 11 is the most potent IKs/s
Structure-based design of nonpeptidic HIV protease inhibitors: The sulfonamide-substituted cyelooctylpyranones
Skulnick, Harvey I.,Johnson, Paul D.,Aristoff, Paul A.,Morris, Jeanette K.,Lovasz, Kristine D.,Howe, W. Jeffrey,Watenpaugh, Keith D.,Janakiraman, Musiri N.,Anderson, David J.,Reischer, Robert J.,Schwartz, Theresa M.,Banitt, Lee S.,Tomich, Paul K.,Lynn, Janet C.,Horng, Miao-Miao,Chong, Kong-Teck,Hinshaw, Roger R.,Dolak, Lester A.,Seest, Eric P.,Schwende, Francis J.,Rush, Bob D.,Howard, Gina M.,Toth, Lisa N.,Wilkinson, Karen R.,Kakuk, Thomas J.,Johnson, Carol W.,Cole, Serena L.,Zaya, Renee M.,Zipp, Gail L.,Possert, Peggy L.,Dalga, Robert J.,Zhong, Wei-Zhu,Williams, Marta G.,Romines, Karen R.
, p. 1149 - 1164 (1997)
Recently, cyclooctylpyranone derivatives with m-carboxamide substituents (e.g. 2c) were identified as potent, nonpeptidic HIV protease inhibitors, but these compounds lacked significant antiviral activity in cell culture. Substitution of a sulfonamide group at the meta position, however, produces compounds with excellent HIV protease binding affinity and antiviral activity. Guided by an iterative structure-based drug design process, we have prepared and evaluated a number of these derivatives, which are readily available via a seven-step synthesis. A few of the most potent compounds were further evaluated for such characteristics as pharmacokinetics and toxicity in rats and dogs. From this work, the p-cyanophenyl sulfonamide derivative 35k emerged as a promising inhibitor, was selected for further development, and entered phase I clinical trials.
Carbocatalytic Cascade Synthesis of Polysubstituted Quinolines from Aldehydes and 2-Vinyl Anilines
Bulatov, Evgeny,Helaja, Juho,Hu, Tao,Lenarda, Anna,M?kel?, Mikko K.,Malinen, Kiia,Melchionna, Michele,Nieger, Martin,Talvitie, Juulia,Wirtanen, Tom
supporting information, p. 3775 - 3782 (2021/07/20)
Oxidized active carbon (oAC) catalyses the formation of polysubstituted quinolines from o-vinyl anilines and aldehydes. The reaction proceeds in a cascade manner through condensation, electrocyclization and dehydrogenation, and gives access to a wide range of quinolines with alkyl and/or aryl substituents as demonstrated with 40 examples. The metal-free catalytic procedure allows a heterogeneous protocol for the synthesis of various polysubstituted quinolines. The mechanistic studies imply that both the acid and quinoidic groups in oAC are integral for the catalytic manifold. (Figure presented.).
Water-Soluble Hypervalent Iodine(III) Having an I-N Bond. A Reagent for the Synthesis of Indoles
Xia, Hai-Dong,Zhang, Yan-Dong,Wang, Yan-Hui,Zhang, Chi
supporting information, p. 4052 - 4056 (2018/07/15)
A readily accessible and bench-stable water-soluble hypervalent iodine(III) reagent (phenyliodonio)sulfamate (PISA) with an I-N bond was synthesized, and its structure was characterized by X-ray crystallography. With PISA, various indoles were synthesized via C-H amination of 2-alkenylanilines involving an aryl migration/intramolecular cyclization cascade with excellent regioselectivity in aqueous CH3CN. Notably, using this new method as the key step, not only two drug molecules, indometacin and zidometacin, but also another bioactive molecule, pravadoline, were synthesized.
INDAZOLE- AND PYRROLOPYRIDINE-DERIVATIVE AND PHARMACEUTICAL USE THEREOF
-
Page/Page column 149, (2013/02/27)
The present invention relates to a novel indazole- or pyrrolopyridine-derivative, represented by the formula (1) below, that has an agonistic action or a partial agonistic action against serotonin-4 receptor, and a pharmaceutical composition comprising the same. Formula (1) [wherein each substituent is as defined in claim 1]
Metal-free intramolecular oxidative decarboxylative amination of primary α-amino acids with product selectivity
Yan, Yizhe,Wang, Zhiyong
, p. 9513 - 9515 (2011/10/01)
A novel metal-free intramolecular oxidative decarboxylative coupling of primary α-amino acids with 2-aminobenzoketones under mild and neutral conditions was developed. Different quinazolines can be selectively obtained by various oxidants.
A simple and efficient approach to the synthesis of 2-phenylquinazolines via sp3 C-H functionalization
Zhang, Jintang,Zhu, Dapeng,Yu, Chenmin,Wan, Changfeng,Wang, Zhiyong
supporting information; experimental part, p. 2841 - 2843 (2010/09/04)
(Figure presented) A facile and novel approach to the synthesis of 2-phenylquinazolines was developed via a tandem reaction following sp 3 C-H functionalization. Twenty-five examples of 2-phenylquinazolines were obtained from easily available 2-aminobenzophenones and benzylic amines with good to excellent yields.
A novel and efficient methodology for the construction of quinazolines based on supported copper oxide nanoparticles
Zhang, Jintang,Yu, Chenmin,Wang, Sujing,Wan, Changfeng,Wang, Zhiyong
supporting information; experimental part, p. 5244 - 5246 (2010/09/05)
A series of quinazolines were synthesized from 2-aminobenzophenones and benzylic amines in good to excellent yields by employing a new heterogeneous catalyst based on the copper oxide nanoparticles supported on kaolin.
Aminophenyl ketone derivatives and a method for the preparation thereof
-
, (2008/06/13)
The present invention provides o-aminophenyl ketone derivatives which are intermediates useful in the manufacture of herbicidal sulfamoyl urea compounds, including the crop selective herbicide 1-{[o-(cyclopropylcarbonyl)phenyl]-sulfamoyl}-3-(4,6-dimethoxy
Aryne intermediates and a process for the preparation thereof
-
, (2008/06/13)
There are provided aryne intermediates of formula I, useful in the manufacture of herbicidal compounds. STR1 Also provided is a method to prepare the formula I intermediates via the palladium catalyzed coupling of an o-halonitrobenzene or o-haloaniline wi
