4294-57-9Relevant articles and documents
Room-Temperature Palladium(II)-Catalyzed Direct 2-Arylation of Indoles with Tetraarylstannanes
Liu, Yuxia,Wang, Chao,Huang, Linjuan,Xue, Dong
supporting information, p. 1613 - 1618 (2020/09/15)
A palladium(II)-catalyzed direct 2-arylation of indoles by tetraarylstannanes with oxygen (balloon) as the oxidant at room temperature has been developed. Various tetraarylstannanes can be employed as aryl sources for 2-arylation of indoles in up to 89% yield, providing a practical and efficient catalytic protocol for accessing 2-arylindoles.
NON-STEROIDAL GLUCOCORTICOID RECEPTOR MODULATORS FOR LOCAL DRUG DELIVERY
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Page/Page column 41, (2017/04/11)
The present invention relates to a compound according to formula (I) wherein R1 is selected from the group consisting of 5- and 6- membered heteroaryl, (C1- C6)alkyl, (C3-C6)cycloalkyl, (4-6)-membered heterocycloalkyl and phenyl; R2 is selected from (C1-C3)alkyl and halo(C1-C3)alkyl; R3 is selected from phenyl, 5-membered heteroaryl and 6-membered heteroaryl; R4 is selected from hydrogen, halogen, (C1- C4)alkyl and halo(C1-C4)alkyl; X1 is selected from CH, C(Rb) and N, X2 is selected from CH and N; Y is selected from -NH- and -O-; m is 0 or 1; n is 0 or 1; L represents a bond, -O-, -NH- or -N(RC)-; or pharmaceutically acceptable salts, hydrates, or solvates thereof. The invention relates further to intermediates for the preparation of said compounds, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases with said compounds, and to the use of said compounds in the manufacture of medicaments.
1,(3,)5-substituted imidazoles, useful in the treatment of hypertension and methods for their preparation
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Paragraph 0171, (2016/03/04)
The present invention provides novel 1,5 and 1,3,5-substituted imidazole compounds in hydrophilic or lipophilic form, which are useful as angiotensin II ATI receptor antagonists suitable for transdermal delivery. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing compounds and their use in methods of treating hypertension and cardiovascular diseases.
Nickel-Catalyzed Asymmetric Kumada Cross-Coupling of Symmetric Cyclic Sulfates
Eno, Meredith S.,Lu, Alexander,Morken, James P.
supporting information, p. 7824 - 7827 (2016/07/11)
Nickel-catalyzed enantioselective cross-couplings between symmetric cyclic sulfates and aromatic Grignard reagents are described. These reactions are effective with a broad range of substituted cyclic sulfates and deliver products with asymmetric tertiary carbon centers. Mechanistic experiments point to a stereoinvertive SN2-like oxidative addition of a nickel complex to the electrophilic substrate.
Palladium-catalyzed aerobic oxidative double allylic C-H oxygenation of alkenes: A novel and straightforward route to α,β-unsaturated esters
Yang, Wanfei,Chen, Huoji,Li, Jianxiao,Li, Chunsheng,Wu, Wanqing,Jiang, Huanfeng
supporting information, p. 9575 - 9578 (2015/06/08)
A mild tandem oxidative functionalization of allyl aromatic hydrocarbons was accomplished using the catalytic system of Pd(OAc)2/DMA under 1 atm O2. The green twofold C-O bond formation involving double allylic C-H oxygenation unlocks opportunities for markedly different synthetic strategies. Moreover, the reaction affords aryl α,β-unsaturated esters directly from readily available terminal olefins in moderate to good yields with excellent chemo- and stereoselectivities.
Bismuth-catalyzed synthesis of polycyclic aromatic hydrocarbons (PAHs) with a phenanthrene backbone via cyclization and aromatization of 2-(2-arylphenyl)vinyl ethers
Murai, Masahito,Hosokawa, Naoki,Roy, David,Takai, Kazuhiko
supporting information, p. 4134 - 4137 (2014/09/30)
The reaction of 2-(2-arylphenyl)vinyl ethers in the presence of a catalytic amount of bismuth(III) triflate gave substituted phenanthrenes in excellent yields under mild reaction conditions. The reaction was also applied to the construction of other polycyclic aromatic hydrocarbons (PAHs), such as chrysene, helicene, and pyrene having a phenanthrene backbone, via regioselective cyclization. This method has the advantages of easy availability of the cyclization precursors, operational simplicity, and high reaction efficiency.
Selective introducing of aryl and amino groups: Reaction of benzanthrone and organometallic reagents
Umeda, Rui,Namba, Teruaki,Yoshimura, Tomohiro,Nakatsukasa, Masamichi,Nishiyama, Yutaka
, p. 1526 - 1531 (2013/02/23)
The reaction of benzanthrone and aryl magnesium bromides produced 6-aryl-substituted benzanthrones in moderate to good yields. Similarly, 6-alkylaminobenzanthrones were selectively prepared by the reaction of benzanthrone and lithium alkylamides. In contrast, for the lithium arylamides, the arylamino groups were selectively introduced at the 4-position of the benzanthrone.
Chemo- and regioselective direct hydroxylation of arenes with hydrogen peroxide catalyzed by a divanadium-substituted phosphotungstate
Kamata, Keigo,Yamaura, Taiyo,Mizuno, Noritaka
supporting information; experimental part, p. 7275 - 7278 (2012/08/28)
Peroxide in, phenol out: The catalyst [-PW10O38V 2(μ-OH)2]3- showed high activity in the hydroxylation of various aromatic compounds with aqueous H2O 2. The system was regioselective, producing para-phenols from monosubstituted benzene derivatives. Furthermore, alkylarenes with reactive side-chain Ca spa 3-H bonds could be chemoselectively hydroxylated without significant formation of side-chain oxygenated products. Copyright
Copper-catalyzed difluoromethylation of β,γ-unsaturated carboxylic acids: An efficient allylic difluoromethylation
He, Zhengbiao,Hu, Mingyou,Luo, Tao,Li, Lingchun,Hu, Jinbo
supporting information, p. 11545 - 11547 (2013/01/15)
Not one but two! A new strategy for the regiospecific construction of compounds with allylic CF2H groups has been developed. The decarboxylative (phenylsulfonyl)difluoromethylation of β,γ- unsaturated carboxylic acids is catalyzed by a Lewis acid (CuCl 2·2 H2O), and the resulting product easily undergoes desulfonylation. Copyright
Cross-coupling of aryl/alkenyl silyl ethers with grignard reagents through nickel-catalyzed CO bond activation
Zhao, Fei,Yu, Da-Gang,Zhu, Ru-Yi,Xi, Zhenfeng,Shi, Zhang-Jie
supporting information; experimental part, p. 1001 - 1003 (2011/12/05)
CO activation and its application have drawn much attention since oxygen-based electrophiles are easily available, less toxic, and more environmentally benign. This letter presents systematically results on the Ni-catalyzed KumadaTamaoCorriu coupling based on siloxy arenes/alkenes, which provides a new strategy of silyl protection/CC bond formation sequence in organic synthesis.
