- General Synthesis of Trialkyl-And Dialkylarylsilylboranes: Versatile Silicon Nucleophiles in Organic Synthesis
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Compared to carbon-based nucleophiles, the number of silicon-based nucleophiles that is currently available remains limited, which significantly hampers the structural diversity of synthetically accessible silicon-based molecules. Given the high synthetic
- Shishido, Ryosuke,Uesugi, Minami,Takahashi, Rikuro,Mita, Tsuyoshi,Ishiyama, Tatsuo,Kubota, Koji,Ito, Hajime
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supporting information
p. 14125 - 14133
(2020/09/16)
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- Metal-Free Electrocatalytic Aerobic Hydroxylation of Arylboronic Acids
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Hydroxylation of arylboronic acids to aryl alcohols was realized by a scalable electrocatalytic method. The present electrochemical hydroxylation employs low-cost methyl viologen as an organic cathodic electrocatalyst and involves O2 as a green and sustainable reactant. The electrochemical kinetic studies shown here can be a powerful tool to gain rich mechanistic and kinetic information and thus an in-depth understanding of the electrocatalytic mechanism.
- Luo, Jian,Hu, Bo,Sam, Alyssa,Liu, T. Leo
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supporting information
p. 361 - 364
(2018/01/28)
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- A specific photosensitizer compound for a target cell.
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PROBLEM TO BE SOLVED: To provide a photosensitization compound which can apply oxidation stress selectively to a target cell, particularly a reporter enzyme expression cell such as β-galactosidase.SOLUTION: A selective photosensitization compound includes a compound represented by general formula (I) or salt thereof, where A represents a univalent group cut by an enzyme; R, R, R, R, R, and Rrepresent a hydrogen atom, a hydroxyl group or the like; and X represents a C-Calkylene group.
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Paragraph 0043; 0044
(2017/08/23)
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- Palladium-catalyzed hydroxylation of aryl and heteroaryl halides enabled by the use of a palladacycle precatalyst
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A method for the hydroxylation of aryl and heteroaryl halides, promoted by a catalyst based on a biarylphosphine ligand tBuBrettPhos (L5) and its corresponding palladium precatalyst (1), is described. The reactions allow the cross-coupling of both potassium and cesium hydroxides with (hetero)aryl halides to afford a variety of phenols and hydroxylated heteroarenes in high to excellent yield.
- Cheung, Chi Wai,Buchwald, Stephen L.
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p. 5351 - 5358
(2014/06/23)
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- Synthesis and SAR of selective small molecule neuropeptide y Y2 receptor antagonists
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Highly potent and selective small molecule neuropeptide Y Y2 receptor antagonists are reported. The systematic SAR exploration of a hit molecule N-(4-ethoxyphenyl)-4-[hydroxy(diphenyl)methyl]piperidine-1-carbothioamide, identified from HTS, led to the discovery of highly potent NPY Y2 antagonists 16 (CYM 9484) and 54 (CYM 9552) with IC50 values of 19 nM and 12 nM respectively.
- Mittapalli, Gopi Kumar,Vellucci, Danielle,Yang, Jun,Toussaint, Marion,Brothers, Shaun P.,Wahlestedt, Claes,Roberts, Edward
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scheme or table
p. 3916 - 3920
(2012/07/03)
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- Model experiments implicate a benzoquinoneketene intermediate in LCP synthesis
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LCP synthesis from 4-hydroxybenzoic acid (HBA) and comonomers involves the formation of phenolic anion end groups at the later stages of polymerization. Model reactions show that these end groups can undergo cleavage to form 4-oxo-2,5-cyclohexadienylideneketene OCK (a benzoquinoneketene intermediate) with loss of a resonance-stabilized phenolic anion. With base, ethyl 4-(4′-hydroxybenzoyloxy)benzoate formed ethyl 4-hydroxybenzoate and poly-HBA, while ethyl 4-(4′-methoxybenzoyloxy)benzoate did not react under the same conditions, indicating an E1cB mechanism involving OCK as an intermediate. Attempted trapping of the OCK intermediate using cycloadditions failed, but it was successfully trapped with secondary amines. These results make it likely that LCP synthesis occurs at least partly via OCK. It is a ubiquitous intermediate in LCP polymerization and characterization.
- Robertson, Jeffrey M.,Contreras, Cristina G.,Bates, Robert B.,Hall
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p. 5586 - 5589
(2012/06/29)
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- PHENOXY-SUBSTITUTED PYRIMIDINES AS OPIOID RECEPTOR MODULATORS
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Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows:wherein R1, Y, R2, R3, and Ra are defined herein.
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Page/Page column 24
(2011/05/08)
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- 1,2,3,4-TETRAHYDROISOQUINOLINE DERIVATIVES, PREPARATIONS THEREOF AND USES THEREOF
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Compounds of general formula (I) wherein D, E, R1, R2, R3, R4, R5, R6 and R7 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
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Page/Page column 44
(2008/06/13)
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- Niobium pentachloride promoted conversion of carboxylic acids to carboxamides: Synthesis of the 4-aryl-1,2,3,4-tetrahydroisoquinoline alkaloid structures
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A practical method for the conversion of carboxylic acids to the corresponding carboxamides mediated by niobium pentachloride under mild conditions is described. The synthesis of the 4-aryl-1,2,3,4-tetrahydroisoquinoline alkaloid structures was accomplished via benzylic lithiation of N-methyl-3,4-dimethoxy-2-(4′-methoxybenzyl)benzamide.
- Nery, Marcelo S.,Ribeiro, Renata P.,Lopes, Claudio C.,Lopes, Rosangela S. C.
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p. 272 - 276
(2007/10/03)
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- Therapeutic amines
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Compounds of formula I, and their pharmaceutically acceptable salts, STR1 in which R1 and R2 are hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, phenylalkyl or alkenyl; or NR1 R2 is a heterocyclic group; A is trimethylene optionally substituted by alkyl and the phenyl ring is optionally substituted by substituents such as halogeno, alkenyl, amino, cyano, ureido, alkyl, carbamoylalkyl, alkanoylamino, alkoxycarbonyl, N-alkyl-alkanoylamino, alkanoyl and amines thereof; are inhibitors of squalene synthese and hence useful in treating diseases in which a lowering of cholesterol is desirable. As well as the use of these compounds in medicine, novel compounds, processes for their preparation and pharmaceutical compositions are also referred to.
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- DIRECTED ORTHO METALATION OF SILYLOXYBENZAMIDES. ANION INDUCED O C SILICON REARRANGEMENT
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Trialkylsilyloxybenzamides 4, o- and m-OSiR3 undergo directed ortho metalation-mediated silicon rearrangement to salicylamides 6, 6- and 3-OH by intra- and inter-molecular mechanisms respectively.
- Billedeau, R.J.,Sibi, M.P.,Snieckus, V.
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p. 4515 - 4518
(2007/10/02)
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- REACTION OF PHENOL WITH DIETHYLCARBAMOYL CHLORIDE IN THE PRESENCE OF LEWIS ACID
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In the presence of either SnCl4 or AlCl3, phenol reacts with diethylcarbamoyl chloride to give phenyl N,N-diethylcarbamate, which undergoes the Fries rearrangement at 170-180 deg C and is capable of being acylated by diethylcarbamoyl chloride in the para position.
- Isakova, A. P.,Naumov, Yu. A.,Nikeryasova, S. V.,Stepanova, A. A.
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p. 1115 - 1119
(2007/10/02)
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