116140-28-4Relevant articles and documents
Preparation of polyfunctional pyridines by a palladium(0)-catalyzed cross-coupling of functionalized aryl Grignard reagents
Bonnet, Véronique,Mongin, Florence,Trécourt, Francois,Quéguiner, Guy,Knochel, Paul
, p. 5717 - 5719 (2001)
Difunctionalized pyridines can be prepared by a Pd(0)-catalyzed cross-coupling of functionalized arylmagnesium compounds with chloro- or bromopyridines at temperatures as low as -40°C. An addition-elimination mechanism involving a palladate intermediate is proposed.
HMPA-catalyzed transfer hydrogenation of 3-carbonyl pyridines and other N-heteroarenes with trichlorosilane
Fu, Yun,Sun, Jian
supporting information, (2019/02/06)
A method for the HMPA (hexamethylphosphoric triamide)-catalyzed metal-freetransfer hydrogenation of pyridines has been developed. The functional group tolerance of the existing reaction conditions provides easy access to various piperidines with ester or ketone groups at the C-3 site. The suitability of this method for the reduction of other N-heteroarenes has also been demonstrated. Thirty-three examples of different substrates have been reduced to designed products with 45–96% yields.
Five-membered azole heterocyclic compound and its preparation method, pharmaceutical composition and use thereof
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Paragraph 0644; 0645; 0646, (2017/02/28)
The present invention relates to a five-membered azole heterocycle compound represented by the following general formula (I), a preparation method of the five-membered azole heterocycle compound, a drug composition of the five-membered azole heterocycle compound, and a use of the five-membered azole heterocycle compound in preparation of drugs for prevention or treatment of TGR5-mediated diseases. The formula (I) is represented by the instruction.
Selective Co/Ti cooperatively catalyzed biaryl couplings of aryl halides with aryl metal reagents
Zeng, Jing,Liu, Kun Ming,Duan, Xin Fang
supporting information, p. 5342 - 5345 (2013/11/06)
Various aryl bromides or chlorides, including those bearing a free COOH, OH, CONHR, and SO2NHR group, coupled with aryl magnesium or lithium reagents in the presence of 7.5 mol % CoCl2/15 mol % PBu3 and substoichiometric Ti(OEt)4 (40 mol % to ArM) at room temperature in high yields with high chemo- and regioslectivity. This simple reaction represents the first example of Co/Ti cooperative catalysis which plays a key role in suppressing undesired homocouplings.
Synthesis and evaluation of a conditionally-silent agonist for the α7 nicotinic acetylcholine receptor
Chojnacka, Kinga,Papke, Roger L.,Horenstein, Nicole A.
, p. 4145 - 4149 (2013/07/26)
We introduce the term 'silent agonists' to describe ligands that can place the α7 nicotinic acetylcholine receptor (nAChR) into a desensitized state with little or no apparent activation of the ion channel, forming a complex that can subsequently generate
5-MEMBERED N-HETEROCYCLIC COMPOUNDS WITH HYPOGLYCEMIC AND HYPOLIPIDEMIC ACTIVITY
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Page 58-59, (2010/02/07)
Use of a compound of the formula: wherein R represents a hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; X represents a bond, an oxygen atom, a sulfur atom, or a group of the formula: -CO-, -CS-, -CR(OR)- or -NR- wherein each of R and R represents a hydrogen atom or a hydrocarbon group which may be substituted, R represents a hydrogen atom or a protective group for a hydroxyl group; m represents an integer of 0 to 3; Y represents an oxygen atom, a sulfur atom, or a group of the formula: -SO-, -SO2-, -NR-, -CONR- or -NRCO- wherein R represents a hydrogen atom or a hydrocarbon group which may be substituted; ring A represents an aromatic ring which may further have 1 to 3 substituents; n represents an integer of 1 to 8; ring B represents a nitrogen-containing 5-membered hetero ring which may further be substituted by an alkyl group; X represents a bond, an oxygen atom, a sulfur atom, or a group of the formula: -SO-, -SO2-, -O-SO2- or -NR- wherein R represents a hydrogen atom or a hydrocarbon group which may be substituted; R represents a hydrogen atom, a hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; W represents a bond or a divalent hydrocarbon residue having 1 to 20 carbon atoms; R represents a group of the formula: -OR (R represents a hydrogen atom or a hydrocarbon group which may be substituted) or -NRR (each of R and R, whether identical or not, represents a hydrogen atom, a hydrocarbon group which may be substituted, a heterocyclic group which may be substituted, or an acyl group which may be substituted; R and R may bind together to form a ring); or a salt thereof, for the manufacture of a pharmaceutical preparation for preventing or treating syndrome X.
Syntheses of substituted pyridines, quinolines and diazines via palladium-catalyzed cross-coupling of aryl Grignard reagents
Bonnet, Véronique,Mongin, Florence,Trécourt, Fran?ois,Quéguiner, Guy,Knochel, Paul
, p. 4429 - 4438 (2007/10/03)
The palladium-catalyzed cross-coupling reactions between arylmagnesium halides (phenylmagnesium chloride, mesitylmagnesium bromide, 4-(methoxycarbonyl)phenylmagnesium chloride and 4-cyanophenylmagnesium chloride) and halopyridines allowed the synthesis of substituted pyridines. Owing to the remarkably mild conditions used (often below 0°C), the reaction could be extended to the use of functionalized halopyridines, haloquinolines and halodiazines.
Derives alkyles et aryles de l'acide nipecotique: synthese et appreciation de l'activite inhibitrice de la capture du GABA en fonction de parametres conformationnels et de biodisponibilite
Lapuyade, Gerard,Schlewer, Gilbert,N'Goka, Victor,Vernieres, Jean-Claude,Chambon, Jean-Pierre,et al.
, p. 383 - 392 (2007/10/02)
Alkyl and aryl derivatives of nipecotic acid: synthesis and inhibition of GABA uptake as a function of conformational parameters and bioavailability.Analogs of nipecotic acid, substituted at positions 2, 3, 4, 5, or 6 with a methyl or phenyl group were pr
