75211-59-5Relevant articles and documents
CARBOXAMIDE OR SULFONAMIDE SUBSTITUTED NITROGEN-CONTAINING 5-MEMBERED HETEROCYCLES AS MODULATORS FOR THE ORPHAN NUCLEAR RECEPTOR ROR GAMMA
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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.
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.
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.
