65117-75-1Relevant academic research and scientific papers
MASP-2 INHIBITORS AND METHODS OF USE
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Paragraph 1675-1676, (2019/12/24)
The present disclosure provides, inter alia, compounds with MASP-2 inhibitory activity, compositions of such compounds and methods of making and using such compounds.
INHIBITORS OF METALLO-BETA-LACTAMASES
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Paragraph 00171; 00172, (2018/12/13)
The present invention relates to compounds of Formula (I) that function as inhibitors of bacterial metallo-beta-lactamases. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of a bacterial infection. (Formula (I))
Ruthenium-catalyzed pyrrole synthesis via oxidative annulation of enamides and alkynes
Li, Bin,Wang, Nuancheng,Liang, Yujie,Xu, Shansheng,Wang, Baiquan
supporting information, p. 136 - 139 (2013/03/28)
An efficient and regioselective ruthenium-catalyzed oxidative annulation of enamides with alkynes via the cleavage of C(sp2)-H/N-H bonds is reported. The reactions can afford N-acetyl substituted or N-unsubstituted pyrroles by altering the reaction conditions slightly.
Mild Rh(III)-catalyzed C-H activation and annulation with alkyne MIDA boronates: Short, efficient synthesis of heterocyclic boronic acid derivatives
Wang, Honggen,Grohmann, Christoph,Nimphius, Corinna,Glorius, Frank
supporting information, p. 19592 - 19595 (2013/02/21)
Taking advantage of Rh(III)-catalyzed C-H activation reactions, we have developed a mild, short, and efficient method for the synthesis of bench-stable 3-isoquinolone MIDA boronates. The reaction is practical and scalable. The product formed has been applied in the Suzuki-Miyaura reaction with high efficiency. This strategy has also been successfully expanded to the synthesis of MIDA boronate functionalized heterocycles such as isoquinoline, pyrrole, and indole.
Rhodium(III)-catalyzed arene and alkene C-H bond functionalization leading to indoles and pyrroles
Stuart, David R.,Alsabeh, Pamela,Kuhn, Michelle,Fagnou, Keith
supporting information; experimental part, p. 18326 - 18339 (2011/03/21)
Recently, the rhodium(III)-complex [Cp*RhCl2]2 1 has provided exciting opportunities for the efficient synthesis of aromatic heterocycles based on a rhodium-catalyzed C-H bond functionalization event. In the present report, the use of complexes 1 and its dicationic analogue [Cp*Rh(MeCN)3][SbF6]2 2 have been employed in the formation of indoles via the oxidative annulation of acetanilides with internal alkynes. The optimized reaction conditions allow for molecular oxygen to be used as the terminal oxidant in this process, and the reaction may be carried out under mild temperatures (60 °C). These conditions have resulted in an expanded compatibility of the reaction to include a range of new internal alkynes bearing synthetically useful functional groups in moderate to excellent yields. The applicability of the method is exemplified in an efficient synthesis of paullone 3, a tetracyclic indole derivative with established biological activity. A mechanistic investigation of the reaction, employing deuterium labeling experiments and kinetic analysis, has provided insight into issues of reactivity for both coupling partners as well as aided in the development of conditions for improved regioselectivity with respect to meta-substituted acetanilides. This reaction class has also been extended to include the synthesis of pyrroles. Catalyst 2 efficiently couples substituted enamides with internal alkynes at room temperature to form trisubstituted pyrroles in good to excellent yields. The high functional group compatibility of this reaction enables the elaboration of the pyrrole products into a variety of differentially substituted pyrroles.
Double diastereoselectivite de la cycloaddition dipolaire-1,3 d'ylures d'azomethine cycliques substitues
Lakhlifi, Tahar,Sedqui, Ahmed,Fathi, Toufik,Laude, Bernard,Robert, Jean-Francois
, p. 1417 - 1423 (2007/10/02)
Seven derivatives of methyl 5-phenyl-3,4-dihydro-2H-pyrrole-2-carboxylates 1 were synthesized.These compounds are precursors of pentagonal cyclic azomethine ylides, the two sides of which are diastereotopic.The 1,3-dipolar species react with N-methyl and
