701-39-3Relevant academic research and scientific papers
Rhodium-Catalyzed Electrooxidative C?H Olefination of Benzamides
Ackermann, Lutz,Struwe, Julia,Zhang, Yan
, p. 15076 - 15080 (2020/06/20)
Metal-catalyzed chelation-assisted C?H olefinations have emerged as powerful tools for the construction of functionalized alkenes. Herein, we describe the rhoda-electrocatalyzed C?H activation/alkenylation of arenes. The olefinations of challenging electron-poor benzamides were thus accomplished in a fully dehydrogenative fashion under electrochemical conditions, avoiding stoichiometric chemical oxidants, and with H2 as the only byproduct. This versatile alkenylation reaction also features broad substrate scope and used electricity as a green oxidant.
Iridium-catalyzed, ligand-controlled directed alkynylation and alkenylation of arenes with terminal alkynes
Sun, Xin,Zhao, Wei,Li, Bi-Jie
supporting information, p. 1298 - 1301 (2020/02/04)
We report iridium-catalyzed C-C formation between benzamides and terminal alkynes. With the choice of a suitable ligand, a C-H alkynylation or alkenylation product could be obtained selectively. The directed C-H alkynylation proceeded without the need for an external oxidant, while the directed C-H alkenylation likely involves an unusual vinylidene mechanism. This divergent reactivity provides access to both alkynylation and alkenylation products from the same set of starting materials.
Ruthenium-Catalyzed Synthesis of N-Methylated Amides using Methanol
Paul, Bhaskar,Panja, Dibyajyoti,Kundu, Sabuj
supporting information, p. 5843 - 5847 (2019/08/26)
An efficient synthesis of N-methylated amides using methanol in the presence of a ruthenium(II) catalyst is realized. Notably, applying this process, tandem C-methylation and N-methylation were achieved to synthesize α-methyl N-methylated amides. In addition, several kinetic studies and control experiments with the plausible intermediates were performed to understand this novel protocol. Furthermore, detailed computational studies were carried out to understand the mechanism of this transformation.
Aerobic thiyl radical addition/cyclization of N-methacryloyl benzamides for the synthesis of isoquinoline-1,3(2H,4H)-dione derivatives
Yuan, Yan-Qin,Kumar, Pailla Santhosh,Zhang, Chun-Niu,Yang, Ming-Hua,Guo, Sheng-Rong
supporting information, p. 7330 - 7338 (2017/09/25)
A highly effective oxidative thiyl radical addition/cyclization of N-methacryloylbenzamides was explored using dioxygen as the sole terminal oxidant without the use of precious and/or toxic transition-metal catalysts. This method provides convenient access to a variety of useful sulfide-containing 4,4-disubstituted isoquinoline-1,3-diones by constructing C-S and C-C bonds in one step.
I2-Catalyzed Oxidative Amidation of Benzylamines and Benzyl Cyanides under Mild Conditions
Nageswara Rao, Sadu,Reddy, N. Naresh Kumar,Samanta, Supravat,Adimurthy, Subbarayappa
, p. 13632 - 13642 (2017/12/26)
We report a novel and efficient method for the oxidation of benzylic carbons (amines and cyanides) into corresponding benzamides using a catalytic amount of I2 and TBHP as the green oxidant via the C-H bond cleavage of the benzylic carbon under mild reaction conditions. According to the literature survey, this is the first report for the oxidative amidation of benzylamines and decyanation of benzyl cyanides in one pot under metal-free conditions.
Re/Mg bimetallic tandem catalysis for [4+2] annulation of benzamides and alkynes via C-H/N-H functionalization
Tang, Qiuzheng,Xia, Dexin,Jin, Xiqing,Zhang, Qing,Sun, Xiao-Qiang,Wang, Congyang
, p. 4628 - 4631 (2013/05/21)
A rhenium-magnesium cocatalyzed [4+2] annulation of benzamides and alkynes via C-H/N-H functionalization is described. The reaction features a divergent and high level of diastereoselectivities, which are readily switchable by subtle tuning of reaction conditions. Thus, a wide range of both cis- and trans-3,4-dihydroisoquinolinones is expediently synthesized in a highly atom-economical manner. Moreover, mechanistic studies unraveled a tandem mode of action between rhenium and magnesium in the catalytic cycles.
Ruthenium-catalyzed oxidative annulation by cleavage of C-H/N-H bonds
Ackermann, Lutz,Lygin, Alexander V.,Hofmann, Nora
, p. 6379 - 6382 (2011/09/12)
Bond activation in action: Unprecedented ruthenium-catalyzed oxidative annulations of alkynes through cleavage of C-H bonds set the stage for an efficient 1(2H)-isoquinolone synthesis with ample scope (see scheme; tAm=tert-amyl). Mechanistic studies provided strong evidence for a rate-limiting C-H bond metalation through carboxylate assistance. Copyright
AZETIDINES AND CYCLOBUTANES AS HISTAMINE H3 RECEPTOR ANTAGONISTS
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Page/Page column 77; 79, (2010/01/29)
The invention relates to compounds of formula (I) wherein R, R0, R1, m, n and X1 to X4 have the meaning as cited in the description and the claims. Said compounds are useful as Histamine H3 receptor antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.
11-BETA-HYDROXYSTEROID DEHYDROGENASE 1 INHIBITORS USEFUL FOR THE TREATMENT OF DIABETES, OBESITY AND DYSLIPIDEMIA
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Page 54, (2010/02/05)
Compounds having Formula (I), including pharmaceutically acceptable salts, hydrates and solvates thereof, are selective inhibitors of the 11β-HSD1 enzyme. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dylsipidemia, hyperlipidemia, hypertension, Syndrome X, and other symptoms associated with NIDDM.
