57381-37-0Relevant articles and documents
Selective synthesis of benzo[4,5]imidazo[2,1-a]isoquinolines via copper-catalyzed tandem annulation of alkynylbenzonitriles with 2-Iodoanilines
Liu, Xiaodong,Deng, Guobo,Liang, Yun
, p. 2844 - 2847 (2018/06/18)
An efficient copper-catalyzed cascade cyclization reaction for selectively synthesizing a variety of benzo[4,5]imidazo[2,1-a]isoquinoline derivatives has been developed. The reaction features the formation of three different C–N bonds in sequence. In the
A radical cyclization cascade of 2-alkynylbenzonitriles with sodium arylsulfinates
Zhou, Bang,Chen, Wenqi,Yang, Yuzhong,Yang, Yuan,Deng, Guobo,Liang, Yun
, p. 7959 - 7963 (2018/11/21)
A convenient radical cyclization cascade procedure for the construction of sulfonated indenones from 2-alkynylbenzonitriles and sodium arylsulfinates has been explored under mild reaction conditions. The present methodology offers a low-cost and operationally straightforward approach to synthesizing various sulfonated indenones in moderate to good yields by simple use of cheap sodium persulfate as an oxidant and environmentally benign water as a co-solvent.
Structure-activity relationships in a novel series of 7-substituted-aryl quinolines and 5-substituted-aryl benzothiazoles at the metabotropic glutamate receptor subtype 5
Zhang, Peng,Zou, Mu-Fa,Rodriguez, Alice L.,Jeffrey Conn,Newman, Amy Hauck
scheme or table, p. 3026 - 3035 (2010/07/06)
The metabotropic glutamate receptor subtype 5 (mGluR5) has been implicated in numerous neuropsychiatric disorders including addiction. We have discovered that the rigid diaryl alkyne template, derived from the potent and selective noncompetitive mGluR5 antagonist 2-methyl-6-(phenylethynyl)pyridine (MPEP), can serve to guide the design of novel quinoline analogues and pharmacophore optimization has resulted in potent mGluR5 noncompetitive antagonists (EC50 range 60-100 nM) in the quinoline series.
Direct N-acetyl enamine formation: Lithium bromide mediated addition of methyllithium to nitriles
Savarin, Cecile G.,Boice, Genevieve N.,Murry, Jerry A.,Corley, Edward,DiMichele, Lisa,Hughes, Dave
, p. 3903 - 3906 (2007/10/03)
An improved protocol for N-acetyl enamine formation is disclosed which involves LiBr-mediated addition of MeLi to substituted nitriles. The resulting enamides are isolated in high yields and excellent purity which permits subsequent hydrogenation at very
An efficient synthesis of a highly functionalized 4-arylpiperidine
Boice, Geneviève N.,Savarin, Cécile G.,Murry, Jerry A.,Conrad, Karen,Matty, Louis,Corley, Edward G.,Smitrovich, Jacqueline H.,Hughes, Dave
, p. 11367 - 11374 (2007/10/03)
In this manuscript, an efficient synthesis of a functionalized 4-arylpiperidine is disclosed. Several synthetic approaches towards formation of the key aryl-piperidine sp3 carbon-carbon bond are discussed, including a scalable route to the piperidine via
Process and intermediates for the preparation of 4-aryl piperidines
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Page 11, (2010/02/08)
A novel process is provided for the preparation of 4-aryl piperidines, and the useful intermediates obtained therein. These compounds are intermediates for the synthesis of melanocortin-4 receptor (MC-4R), which are useful for the treatment of disorders such as obesity, diabetes, male sexual dysfunction, and female sexual dysfunction.
Angiotensin II antagonizers which are condensed pyridine derivatives
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, (2008/06/13)
The invention concerns pharmaceutically useful novel compounds of the formula I, in which R1, R2, R3, R4, R5, R6, R7, X and Z have the various meanings defined herein, and their non-toxic salts, and pharmaceutical compositions containing them. The novel compounds are of value in treating conditions such as hypertension and congestive heart failure. The invention further concerns processes for the manufacture of the novel compounds and the use of the compounds in medical treatment.