75211-59-5Relevant academic research and scientific papers
CARBOXAMIDE OR SULFONAMIDE SUBSTITUTED NITROGEN-CONTAINING 5-MEMBERED HETEROCYCLES AS MODULATORS FOR THE ORPHAN NUCLEAR RECEPTOR ROR GAMMA
-
Page/Page column 123-124, (2014/03/21)
The invention provides modulators for the orphan nuclear receptor RORy and methods for treating RORy mediated diseases by administering these novel RORy modulators to a human or a mammal in need thereof. Specifically, the present invention provides carboxamide containing cyclic compounds of Formula (1) to Formula (5) and the enantiomers, diastereomers, tautomers, /V-oxides, solvates and pharmaceutically acceptable salts thereof.
Synthesis of some diethylphosphono substituted 3H-pyrrolizines
Loussouarn,Servant,Guervenou,Sturtz
, p. 275 - 285 (2007/10/03)
The preparation of various alkyl substituted monophosphonate 3H-pynolizines via a tandem Michael □ Horner-Emmons reaction is reported. These products were prepared from tetraethyl ethylidene gem-bisphosphonate and corresponding 2-acylpyrroles.
2-SUBSTITUTED 1,3-BENZODITHIOLIUM TETRAFLUOROBORATES AS USEFUL ACYLATING AGENTS OF PYRROLE
Barbero, Margherita,Cadamuro, Silvano,Degani, Iacopo,Dughera, Stefano,Fochi, Rita,et al.
, p. 619 - 627 (2007/10/02)
A comparative study on the acylation of pyrrole by utilizing 2-substituted 1,3-benzodithiolium tetrafluoroborates instead of 2-substituted 1,3-benzoxathiolium tetrafluoroborates has been accomplished.The use of 2-substituted 1,3-benzodithiolium tetrafluoroborates proved to be more convenient since it gives higher yields of 2-acylpyrroles (58-90percent) and appears of larger applicability for the preparation of symmetrical and unsymmetrical 2,5-diacylpyrroles which were obtained in most cases in quantitative yields.
Ruthenium Complex Catalyzed Intermolecular Hydroacylation and Transhydroformylation of Olefins with Aldehydes
Kondo, Teruyuki,Akazome, Motohiro,Tsuji, Yasushi,Watanabe, Yoshihisa
, p. 1286 - 1291 (2007/10/02)
Low-valent ruthenium complexes such as dodecacarbonyltriruthenium (Ru3(CO)12), (η4-1,5-cyclooctadiene)(η6-1,3,5-cyclooctatriene)ruthenium (Ru(COD)(COT)) and bis(η5-cyclooctadienyl)ruthenium showed high catalytic activity for the intermolecular hydroacylation of olefins with various aromatic and heteroaromatic aldehydes at 180-200 deg C for 24-48 h under an initial carbon monoxide pressure of 20 kg cm-2 to give unsymmetric ketones in moderate to good yields.In the reaction of 2-thiophenecarbaldehyde with cyclohexene, cyclohexyl 2-thienyl ketone was obtained in 62 percent yield.On the other hand, when the aliphatic aldehyde, heptanal, was treated with cyclohexene, the corresponding ketone was not obtained at all, and a transhydroformylation reaction proceeded; i.e., the formyl group of heptanal was apparently transformed to cyclohexene to give cyclohexanecarbaldehyde in 29 percent yield, together with their Tishchenko-type reaction products.
Acylation of Pyrrole and N-Methylpyrrole with 1,3-Benzoxathiolium Tetrafluroborates. A High-Yield Method for the Synthesis of Diacylpyrroles
Barbero, Margherita,Cadamuro, Silvano,Degani, Iacopo,Fochi, Rita,Gatti, Antonella,Regondi, Valeria
, p. 2245 - 2250 (2007/10/02)
2-Substituted 1,3-benzoxathiolium tetrafluoroborates (I) were used as masked acylating agents for pyrrole and N-methylpyrrole.The reactions on pyrrole (II) were regiospecific, and according to the molar ratio of the reagents (I:II = 1:3 or 2.5-3:1), 2-acylpyrroles were obtained in moderate to good yields (38-82percent) and 2,5-diacylpyrroles were obtained in excellent yields (in most cases, quantitative).The reactions on N-methylpyrrole (III) were not regioselective, and both α- and β-positions were attacked.So, depending on the molar ratio of the reagents (I:III = 1:3 or 2,5-3:1), 2- and 3-acyl-N-methylpyrroles (9-51percent and 27-68percent yields, respectively) and 2,4- and 2,5-diacyl-N-methylpyrroles (60-93percent and 17-40percent, respectively) were obtained.A very interesting feature of the new method is the possibility of introducing two identical or different acyl groups in the pyrrole ring under mild conditions. 1H and 13C NMR spectra of all the new compounds and IR spectra, recorded in the gas phase, of 2- and 3-acylpyrroles and of 2,4- and 2,5-diacylpyrroles are reported.
An Efficient Synthesis of 2-Acylpyrroles
Nakahara, Yoshiaki,Fujita, Akira,Ogawa, Tomoya
, p. 1491 - 1496 (2007/10/02)
Pyrrolylmagnesium bromide reacted with thiol- and selenolesters in the presence of cuprous iodide to afford 2-acylpyrroles regioselectively.
5-Substituted 2-pyrroleglyoxylic acids, 5-substituted 2-pyrrolylglycines and derivatives thereof
-
, (2008/06/13)
5-Substituted 2-pyrroleglyoxylic acids, L- and DI-5-substituted 2-pyrrolylglycines and their derivatives of the formulae STR1 and pharmaceutically acceptable cationic and acid addition salts thereof, wherein R is hydrogen or alkyl having from one to four
