71095-49-3Relevant academic research and scientific papers
Synthesis of Amides and Esters by Palladium(0)-Catalyzed Carbonylative C(sp3)?H Activation
?arny, Tomá?,Baudoin, Olivier,Clemenceau, Antonin,Rocaboy, Ronan
supporting information, p. 18980 - 18984 (2020/09/01)
The 1,4-palladium shift strategy allows the functionalization of remote C?H bonds that are difficult to reach directly. Reported here is a domino reaction proceeding by C(sp3)?H activation, 1,4-palladium shift, and amino- or alkoxycarbonylation, which generates a variety of amides and esters bearing a quaternary β-carbon atom. Mechanistic studies showed that the aminocarbonylation of the σ-alkylpalladium intermediate arising from the palladium shift is fast using PPh3 as the ligand, and leads to the amide rather than the previously reported indanone product.
SUBSTITUTED TETRAHYDROISOQUINOLINE COMPOUNDS AS FACTOR XIA INHIBITORS
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Paragraph 00303, (2013/04/25)
The present invention provides compounds of Formula (I) or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor XIa and/or plasma kallikrein which may be used as medicaments.
Metal-free synthesis of polysubstituted pyrroles by (diacetoxyiodo)benzene- mediated cascade reaction of 3-alkynyl amines
Mo, Dong-Liang,Ding, Chang-Hua,Dai, Li-Xin,Hou, Xue-Long
supporting information, p. 3200 - 3204 (2013/01/12)
Free metal jacket: A regioselective metal-free synthesis of polysubstituted pyrroles has been developed through a (diacetoxyiodo)benzene-mediated cascade reaction of alkynyl amines in moderate to good yield (see scheme).
Copper(I)-assisted mild and convenient synthesis of new Se-N heterocycles: Access to a promising class of GPx mimics
Erdelmeier,Tailhan-Lomont,Yadan
, p. 8152 - 8157 (2007/10/03)
Benzisoselenazolines 15 and benzisoselenazines 21, designed as low molecular weight mimics of glutathione peroxidases, were synthesized for the first time. Starting from amines 13 and 14, a smooth introduction of selenium in nonactivated aryl bromides using KSeCN in the presence of CuI was developed. An equimolar quantity of CuI and the presence of Et3N as a base are necessary to achieve a complete conversion of the starting material. The reaction is feasible in various solvents such as DMF, acetonitrile, and THF. The desired new Se-N heterocycles 15 and 21 were isolated under optimized conditions in yields of 82 and 68%, respectively. Experiments have been conducted with various copper(I) and copper(II) salts, a chloroamine 17, an aryl bromide 18, and an N-acylated amine 19 to show the scope and the limitations of this method. The previously unknown sulfur analogues 20 and 22 have been synthesized in moderate yields using a slightly modified procedure. Finally, a mechanistic scheme has been proposed to discuss some interesting findings, which were obtained during the optimization process of this new introduction of selenium.
Compounds having a benzisoselen-azoline and -azine structure, method for preparing same and therapeutic uses thereof
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, (2008/06/13)
The invention concerns novel benzisoselen-azoline and -azine derivatives. These novel derivatives have the following general formula (II): STR1 where: R1 to R8 and R10 have various meanings, in particular H, alkyl, etc . .
