41996-96-7Relevant academic research and scientific papers
A nitric oxide donor nature of the benzofuran compounds (by machine translation)
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Paragraph 0063-0064, (2017/04/20)
The invention discloses a benzofuran compound with nitrous oxide donor property. The benzofuran compound is a compound shown by a general formula (I) or a pharmaceutically acceptable salt thereof, wherein in the formula, R1 or R2 represents independent hy
Mechanism of the TiIII-Catalyzed Acyloin-Type Umpolung: A Catalyst-Controlled Radical Reaction
Streuff, Jan,Feurer, Markus,Frey, Georg,Steffani, Alberto,Kacprzak, Sylwia,Weweler, Jens,Leijendekker, Leonardus H.,Kratzert, Daniel,Plattner, Dietmar A.
supporting information, p. 14396 - 14405 (2015/12/01)
The titanium(III)-catalyzed cross-coupling between ketones and nitriles provides an efficient stereoselective synthesis of α-hydroxyketones. A detailed mechanistic investigation of this reaction is presented, which involves a combination of several methods such as EPR, ESI-MS, X-ray, in situ IR kinetics, and DFT calculations. Our findings reveal that C-C bond formation is turnover-limiting and occurs by a catalyst-controlled radical combination involving two titanium(III) species. The resting state is identified as a cationic titanocene-nitrile complex and the beneficial effect of added Et3N·HCl on yield and enantioselectivity is elucidated: chloride coordination initiates the radical coupling. The results are fundamental for the understanding of titanium(III)-catalysis and of relevance for other metal-catalyzed radical reactions. Our conclusions might apply to a number of reductive coupling reactions for which conventional mechanisms were proposed before.
Direct synthesis of water-tolerant alkyl indium reagents and their application in palladium-catalyzed couplings with aryl halides
Shen, Zhi-Liang,Goh, Kelvin Kau Kiat,Yang, Yong-Sheng,Lai, Yin-Chang,Wong, Colin Hong An,Cheong, Hao-Lun,Loh, Teck-Peng
supporting information; experimental part, p. 511 - 514 (2011/03/17)
A direct result: Alkyl indium reagents are synthesized by the insertion of indium into alkyl halide mediated by CuCl. The synthetic utility of these reagents is demonstrated by their palladium-catalyzed coupling with aryl halides (see scheme). The reagents are compatible with various functional groups, and this makes the protocol generally useful in organic synthesis. DMA=N,N-dimethylacetamide, TBS=tert-butyldimethylsilyl.
Self-limiting robust surface-grafted organic nanofilms
Todd Banner,Tekobo, Samuel,Garay, Fernando,Clayton, Benjamin T.,Thomas, Zachary P.,Lindner, Ernoe,Richter, Andrew G.,Pinkhassik, Eugene
experimental part, p. 2248 - 2254 (2011/11/30)
Robust surface-bound insulating polymer films with controlled thickness in 5 nm range are important for technological advances in diverse disciplines such as electrochemical sensors, molecular electronics, separations, and anticorrosive coatings. Creatin
One-pot synthesis of symmetrical 1,3-diarylureas or substituted benzamides directly from benzylic primary alcohols and effective oxidation of secondary alcohols to ketones using phenyliodine diacetate in combination with sodium azide
Li, Xiao-Qiang,Wang, Wei-Kun,Han, Yi-Xin,Zhang, Chi
experimental part, p. 2588 - 2598 (2010/12/25)
Benzylic primary alcohols can be directly converted into symmetrical 1,3-diarylureas or substituted benzamides via an one-pot oxidative reaction using the combined reagent of phenyliodine diacetate and sodium azide. This new reaction constitutes a step-economical way to prepare symmetric 1,3-diarylureas or substituted benzamides depending upon the substituents on the phenyl rings of starting alcohols. The sodium acetate generated in situ from the ligand exchange between phenyliodine diacetate and sodium azide plays the pivotal role in the formation of 1,3-diarylureas. In addition, it is also found that various secondary alcohols can be readily oxidized to their corresponding ketones in excellent yields using the same reagent system of phenyliodine diacetate and sodium azide. Generally, secondary alcohols are preferentially oxidized to the corresponding ketones in the presence of primary ones with the limited amounts of phenyliodine diacetate and sodium azide.
Pharmacophore and structure-activity relationships of integrase inhibition within a dual inhibitor scaffold of HIV reverse transcriptase and integrase
Wang, Zhengqiang,Tang, Jing,Salomon, Christine E.,Dreis, Christine D.,Vince, Robert
experimental part, p. 4202 - 4211 (2010/09/12)
Rational design of dually active inhibitors against human immunodeficiency virus (HIV) reverse transcriptase (RT) and integrase (IN) has proved viable with 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT) type of non-nucleoside RT inhibitors (NNRTIs). To establish the pharmacophore and study the structure-activity relationships (SAR) of integrase inhibition within a previously disclosed RT/IN dual inhibitor scaffold, new analogues featuring substitution at different sites of the HEPT ring were designed and synthesized. These studies have revealed an IN inhibition pharmacophore that is merged with the known RT pharmacophore through a shared C-6 benzyl group. Further SAR also demonstrated that optimal IN inhibition within our dual inhibitor scaffold requires a regiospecific (N-1) diketoacid (DKA)-carrying pendant with a certain length.
One-pot synthesis of carbamoyl azides directly from primary alcohols and oxidation of secondary alcohols to ketones using iodobenzene dichloride in combination with sodium azide
Li, Xiao-Qiang,Wang, Wei-Kun,Zhang, Chi
scheme or table, p. 2342 - 2350 (2009/12/27)
An effective synthesis of carbamoyl azides directly from primary alcohols using iodobenzene dichloride in combination with sodium azide has been developed. Moreover, the same regent combination was also efficient for the oxidation of secondary alcohols to the corresponding ketones.
Design of new potent and selective secretory phospholipase A2 inhibitors. Part 5: Synthesis and biological activity of 1-alkyl-4-[4,5-dihydro-1,2,4-[4H]-oxadiazol-5-one-3-ylmethylbenz-4′-yl(oyl)] piperazines
Boukli, Latifa,Touaibia, Mohamed,Meddad-Belhabich, Nadia,Djimde, Atime,Park, Chang-Ha,Kim, Jung-Joo,Yoon, Joo-Hyoung,Lamouri, Aazdine,Heymans, Francoise
, p. 1242 - 1253 (2008/09/17)
Among the different PLA2s identified to date, the group IIA secretory PLA2 (sPLA2 GIIA) is implied in diverse pathological conditions. In this work we describe the synthesis, inhibitory activities, and structure-activity relationships (SAR) of a new class of substituted piperazine derivatives. The in vitro fluorimetric assay using two groups of enzymes, GIB and GIIA, revealed several compounds as highly potent inhibitors (IC50 = 0.1 μM). The in vivo activity assessed by ip or per os administration in a carrageenan-induced edema test in rats showed that two compounds proved to be as potent as indomethacin (10 mg/kg).
Novel inhibitor compounds specific of secreted non-pancreatic human a2phospholipase of group II
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Page/Page column 12, (2010/02/11)
The present invention relates to a compound of the following formula (I) and pharmaceutical compositions containing the compound of formula (I): wherein D, Y, A, B, p, q, W and R have the same meanings as defined in the specification.
8-Phenyl-Substituted Dipyrromethene·Bf2 Complexes as Highly Efficient and Photostable Laser Dyes
Garcia-Moreno,Costela,Campo,Sastre,Amat-Guerri,Liras,Lopez Arbeloa,Banuelos Prieto,Lopez Arbeloa
, p. 3315 - 3323 (2007/10/03)
We report on the synthesis and the photophysical and lasing properties of two new dipyrromethene·BF2 dyes, analogues of the commercial dye PM567, dissolved in liquid solutions or in polymeric matrices of poly(methyl methacrylate) and as solid c
