52568-28-2Relevant academic research and scientific papers
Stereoselective Synthesis of Chiral β-Fluoro α-Amino Acids via Pd(II)-Catalyzed Fluorination of Unactivated Methylene C(sp3)-H Bonds: Scope and Mechanistic Studies
Zhang, Qi,Yin, Xue-Song,Chen, Kai,Zhang, Shuo-Qing,Shi, Bing-Feng
, p. 8219 - 8226 (2015)
The synthesis of fluorinated complex molecules via direct C(sp3)-H fluorination is attractive yet remains challenging. Here we describe the Pd(II)-catalyzed fluorination of unactivated methylene C(sp3)-H bonds by an inner-sphere mech
Nickel-catalyzed ortho-halogenation of unactivated (hetero)aryl C-H bonds with lithium halides using a removable auxiliary
Zhan, Bei-Bei,Liu, Yan-Hua,Hu, Fang,Shi, Bing-Feng
, p. 4934 - 4937 (2016)
The first example of Ni-catalyzed halogenation of (hetero)aryl C-H bonds with lithium halides (LiX, X = Br, I, Cl) using PIP as a removable directing group is reported. This protocol provides an efficient access to ortho-halogenated (hetero)arenes with operational simplicity, good functional group tolerance, and large-scale synthesis.
Copper-Mediated Thiolation of Unactivated Heteroaryl C?H Bonds with Disulfides under Ligand- and Metal-Oxidant-Free Conditions
Li, Ya,Liu, Yue-Jin,Shi, Bing-Feng
, p. 4117 - 4121 (2017)
Various sulfenylated heteroarenes were synthesized by a copper-mediated C?H thiolation, which was assisted by a 2-(pyridin-2-yl)isopropylamine (PIP-amine) directing group. The reaction features a broad substrate scope, good functional group tolerance, ligand- and metal-oxidant-free conditions, exceptional compatibility with aliphatic disulfides, and excellent yields, providing a highly efficient approach to the biologically important sulfenylated heteroarenes. (Figure presented.).
5-FLUORONICOTINAMIDE DERIVATIVES AND USES THEREOF
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Paragraph 00495-00498, (2021/04/10)
Provided herein is a compound of Formula (I), or pharmaceutically acceptable salt thereof, wherein R1, Y, X, and n are defined herein. Also provided herein are compositions comprising a compound of Formula (I) or pharmaceutically acceptable salt thereof, and methods of using a compound of Formula (I) or pharmaceutically acceptable salt thereof, e.g., in the treatment of heart disease.
HETEROCYCLIC COMPOUNDS AS ADENOSINE ANTAGONISTS
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Paragraph 0405-0406, (2020/08/05)
Aminopyrazine compounds as modulators of an adenosine receptor are provided. The compounds may find use as therapeutic agents for the treatment of diseases mediated through a G-protein-coupled receptor signaling pathway and may find particular use in onco
Access to β-Ketonitriles through Nickel-Catalyzed Carbonylative Coupling of α-Bromonitriles with Alkylzinc Reagents
Donslund, Aske S.,Neumann, Karoline T.,Corneliussen, Nicklas P.,Grove, Ebbe K.,Herbstritt, Domenique,Daasbjerg, Kim,Skrydstrup, Troels
supporting information, p. 9856 - 9860 (2019/07/09)
Herein, we report a nickel-catalyzed carbonylative coupling of α-bromonitriles and alkylzinc reagents with near stoichiometric carbon monoxide to give β-ketonitriles in good yields. The reaction is catalyzed by a readily available and stable nickel(II) pincer complex. The developed protocol tolerates substrates bearing a variety of functional groups, which would be problematic or incompatible with previous synthetic methods. Additionally, we demonstrate the suitability of the method for carbon isotope labeling by the synthesis of 13C-labeled β-ketonitriles and their transformation into isotopically labeled heterocycles.
Palladium-Catalyzed Electrochemical C-H Bromination Using NH4Br as the Brominating Reagent
Yang, Qi-Liang,Wang, Xiang-Yang,Wang, Tong-Lin,Yang, Xiang,Liu, Dong,Tong, Xiaofeng,Wu, Xin-Yan,Mei, Tian-Sheng
supporting information, p. 2645 - 2649 (2019/04/17)
The palladium-catalyzed electrochemical C-H bromination of benzamide derivatives under divided cells is developed, in which NH4Br serves as a brominating reagent and electrolyte. The protocol avoids the use of chemical oxidants and provides an alternative method for the synthesis of aryl bromides.
Nickel-Catalyzed Sulfonylation of C(sp2)–H Bonds with Sodium Sulfinates
Liu, Shuang-Liang,Li, Xue-Hong,Zhang, Shu-Sheng,Hou, Sheng-Kai,Yang, Guang-Chao,Gong, Jun-Fang,Song, Mao-Ping
supporting information, p. 2241 - 2246 (2017/07/07)
The first nickel-catalyzed ortho-sulfonylation of C(sp2)–H bonds with sodium sulfinates directed by (pyridin-2-yl)isopropylamine (PIP-amine) is described. This strategy exhibits a broad substrate scope and good functional group tolerance with high monosulfonylation selectivity. Besides arenes and heteroarenes, the reaction can also be extended to alkenes, providing diverse diaryl and alkyl aryl sulfones in high yields. Furthermore, a plausible Ni(I)/Ni(III) mechanism is outlined based on our experimental results and related precedents. (Figure presented.).
NITROGEN-CONTAINING SATURATED HETEROCYCLIC COMPOUND
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Paragraph 0344, (2016/08/29)
The present invention provides a compound represented by the following formula (I) or its pharmaceutically acceptable salt: [wherein, R1 represents optionally substituted C1-4 alkyl, n shows integer of 1 to 4, R2 represents optionally substituted C1-4 alkyl or hydrogen atom, R3 represents optionally substituted C1-4 alkyl, R4a, R4b, R4c, and R4d, similarly or differently, represent optionally substituted C6-14 aryl, optionally substituted C1-4 alkyl, or hydrogen atom and the like, A represents optionally substituted C6-14 aryl or optionally substituted 5 to 11 membered heteroaryl].
Dual Role of Acetate in Copper(II) Acetate Catalyzed Dehydrogenation of Chelating Aromatic Secondary Amines: A Kinetic Case Study of Copper-Catalyzed Oxidation Reactions
Sreenath, Kesavapillai,Yuan, Zhao,Macias-Contreras, Miguel,Ramachandran, Vasanth,Clark, Ronald J.,Zhu, Lei
, p. 3728 - 3743 (2016/08/19)
Copper(II) acetate is a frequent empirical choice of the copper source in copper(II)-mediated redox reactions. The effect of the acetate counterion appears crucial but has not been adequately investigated. Herein, we report that copper(II) acetate catalyz
