126370-67-0Relevant articles and documents
NEW BENZAMIDE DERIVATIVES AS PPAR-GAMMA MODULATORS
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Paragraph 0097-0098; 0102-0103, (2019/06/27)
The present invention relates to novel benzamides derivatives of formula (I) as modulators of PPAR-gamma receptor, to processes for their preparation, to pharmaceutical compositions comprising said compounds and to said compound for use in the treatment of pathological conditions, disorders or diseases that can improve by modulation of PPAR-gamma receptor, such as cancer; metabolic diseases, inflammatory diseases, respiratory disorders, autoimmune diseases, neurodegenerative diseases, cardiovascular diseases and renal diseases.
Pd-Catalyzed Suzuki coupling reactions of aryl halides containing basic nitrogen centers with arylboronic acids in water in the absence of added base
Li, Zhao,Gelbaum, Carol,Campbell, Zachary S.,Gould, Paul C.,Fisk, Jason S.,Holden, Bruce,Jaganathan, Arvind,Whiteker, Gregory T.,Pollet, Pamela,Liotta, Charles L.
supporting information, p. 15420 - 15432 (2017/12/15)
The Pd-catalyzed Suzuki coupling reactions of a series of aryl chlorides and aryl bromides containing basic nitrogen centers with arylboronic acids in water in the absence of added base are reported. The reactions proceed either partially or entirely under acidic conditions. After surveying twenty-two phosphorus ligands, high yields of products were obtained with aryl chlorides only when a bulky ligand, 2-(di-tert-butyl-phosphino)-1-phenyl-1H-pyrrole (cataCXiumPtB) was used. In contrast, aryl bromides produced high yields of products in the absence of both added base and added ligand. In order to explore the Suzuki coupling process entirely under acidic conditions, a series of reactions were conducted in buffered acidic media using several model substrates. 4-Chlorobenzylamine, in the presence of cataCXiumPtB, produced high yields of product at buffered pH 6.0; the yields dropped off precipitously at buffered pH 5.0 and lower. The fall-off in yield was attributed to the decomposition of the Pd-ligand complex due to the protonation of the ligand in the more acidic aqueous media. In contrast, in the absence of an added ligand, 4-amino-2-chloropyridine produced quantitative yields at buffered pH 3.5 and 4.5 while 4-amino-2-bromopyridine produced quantitative yields in a series of buffered media ranging from pH 4.5 to 1.5. These substrates are only partially protonated in acidic media and can behave as active Pd ligands in the Suzuki catalytic cycle.
POPd/TBAB co-catalyzed Suzuki cross-coupling reaction of heteroaryl chlorides/bromides with 4-fluorophenylboronic acid in water
Li, Ben,Zhang, Zhiqiang
, p. 637 - 644 (2016/02/19)
An organic solvent free and efficient heterogeneous synthesis for bridging heteroaryl halides and 4-fluorophenylboronic acid was studied in aqueous media according to the Suzuki cross-coupling protocol. High yields of heteroaryl-aryl fluorides were successfully obtained with: chloro-/bromo-substituted pyridine, thiophene, indole, and inzole in neat water using palladium phosphinous acid complexes (POPd)/tetrabutylammonium bromide (TBAB) as co-catalysts. A possible mechanism for the heterogeneous coupling reaction is proposed and discussed according to the function of the TBAB interphases. The notable properties of the reported method are highly co-catalytic activity, hetero-atom tolerance, simple separating procedure and little environmental disposal impact.