- Synthesis and biological evaluation of a novel photo-activated histone deacetylase inhibitor
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Hydroxamic acid-based histone deacetylase inhibitors (HDACi) are a class of epigenetic agents with potentially broad therapeutic application to several disease states including post angioplasty mediated neointimal hyperplasia (NIH). Precise spatiotemporal
- Dear, Anthony E.,Liu, Hongbin,Mountford, Simon,Robinson, Andrea,Sama, Gopal R.,Thompson, Phillip
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supporting information
(2020/06/05)
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- HEPATITIS B CORE PROTEIN ALLOSTERIC MODULATORS
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ABSTRACT The present disclosure provides, in part, compounds having allosteric effector properties against Hepatitis B virus Cp. Also provided herein are methods of treating viral infections, such as hepatitis B, comprising administering to a patient in need thereof a disclosed compound.
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Paragraph 000404
(2015/10/05)
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- Aryldiazonium Tetrafluoroborate Salts as Green and Efficient Coupling Partners for the Suzuki-Miyaura Reaction: From Optimisation to Mole Scale
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The use of aryldiazonium tetrafluoroborate salts as coupling partners in the Suzuki-Miyaura reaction was investigated from a process chemistry perspective including safety evaluation, solvent and catalyst screening and multivariate factor optimisation. Optimised conditions were applied to a range of substrates to evaluate the scope and limitations of the reaction, and one example was carried out on mole scale to demonstrate the practicality and scalability of the process.
- Colleville, Aymeric P.,Horan, Richard A. J.,Tomkinson, Nicholas C. O.
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supporting information
p. 1128 - 1136
(2015/04/22)
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- Improved Suzuki-Miyaura reactions of aryldiazonium salts with boronic acids by tuning palladium on charcoal catalyst properties
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An improved Suzuki-Miyaura cross-coupling reaction of aryldiazonium tetrafluoroborates with boronic acids catalyzed by a highly active palladium catalyst supported on charcoal is described as an extremely practical and efficient protocol. A properties-activity study of various catalysts clearly established that the optimal catalytic activity was obtained with palladium nanoparticles having a low oxidation degree and uniformly dispersed on the charcoal. The optimized reaction conditions allow the cross-coupling to proceed at room temperature without any base and ligand in technical grade methanol. Although the catalyst could not be recycled, the low palladium contamination of the solvent and product after a simple filtration of the palladium on charcoal (Pd/C) renders the present protocol competitive and safer for the environment compared to more conventional homogeneous conditions. We have highlighted the efficiency of this novel protocol by a short synthesis of the fungicide Boscalid
- Felpin, Francois-Xavier,Fouquet, Eric,Zakri, Cecile
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experimental part
p. 649 - 655
(2009/12/08)
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- Fast Suzuki-Miyaura cross-coupling reaction with hexacationic triarylphosphine Bn-dendriphos as ligand
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The application of hexa[(dimethylamino)-methyl]-functionalized triphenylphosphine (1) and its benzylammonium salt, Bn-Dendriphos (2), in the Suzuki-Miyaura cross-coupling of aryl bromides with arylboronic acids is described. The 3,5-bis[(benzyldimethylammonio)methyl] substitution pattern in 2 leads to a rate enhancement compared to both the non-ionic parent compound 1 and triphenylphospine (PPh3) itself. At the same time, the resulting catalytic species are stable towards palladium black formation, even at a phosphine/palladium ratio of 1. These observations are attributed to the presence of a total of six ammonium groups in the backbone of the phosphine ligand, which presumably leads to an unsaturated phosphine-palladium complex.
- Snelders, Dennis J. M.,Kreiter, Robert,Firet, Judith J.,Van Koten, Gerard,Gebbink, Robertus J. M. Klein
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experimental part
p. 262 - 266
(2009/04/07)
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- Biarylaniline phenethanolamines as potent and selective β3 adrenergic receptor agonists
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The synthesis of a series of phenethanolamine aniline agonists that contain an aniline ring on the right-hand side of the molecule substituted at the meta position with a benzoic acid or a pyridyl carboxylate is described. Several of the analogues (e.g.,
- Uehling, David E.,Shearer, Barry G.,Donaldson, Kelly H.,Chao, Esther Y.,Deaton, David N.,Adkison, Kim K.,Brown, Kathleen K.,Cariello, Neal F.,Faison, Walter L.,Lancaster, Mary E.,Lin, Jasmine,Hart, Robert,Milliken, Tula O.,Paulik, Mark A.,Sherman, Bryan W.,Sugg, Elizabeth E.,Cowan, Conrad
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p. 2758 - 2771
(2007/10/03)
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- Therapeutic biaryl derivatives
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The present invention relates to therapeutic biaryl derivatives of formula (I), and pharmaceutically acceptable derivatives thereof wherein R1is a phenyl, naphthyl, pyridyl, thiazolyl, phenoxymethyl, or pyrimidyl group, optionally substituted by one or more substituents selected from the group consisting of halogen, hydroxy, C1-6alkoxy, C1-6alkyl, nitro, cyano, hydroxymethyl, trifluoromethyl, —NR6R6, and —NHSO2R6, where each R6is independently hydrogen or C1-4alkyl; R2is hydrogen or C1-6alkyl; X is oxygen, sulfur, —NH, or —NC1-4alkyl; R3is cyano, tetrazol-5-yl, or —CO2R7where R7is hydrogen or C1-6alkyl; R4and R5are independently hydrogen, C1-6alkyl, —CO2H, —CO2C1-6alkyl, cyano, tetrazol-5-yl, halogen, trifluoromethyl, or C1-6alkoxy, or, when R4and R5are bonded to adjacent carbon atoms, R4and R5may, together with the carbon atoms to which they are bonded, form a fused5or6membered ring optionally containing one or two nitrogen, oxygen, or sulfur atoms; and Y is N or CH, to processes for their preparation and their use in the treatment of diseases susceptible to ameleoration by treatment with a beta-3adrenoceptor agonist.
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- Thiazolopyrimidine derivatives
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Thiazolopyrimidine derivatives represented by the formula STR1 and salts thereof are provided, which are characterized by a carboxamide residue substituted with R4 and R5. The derivatives and salts thereof exhibit antiangiogenic acti
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- The Effects of Substituents on the Rate of Saponification of Biphenyl-4-carboxylates
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Second-order rate constants have been measured for the saponification of methyl 2'-, 3'-, and 4'-substituted biphenyl-4-carboxylates at several temperatures in 85percent (w/w) methanol-water and activation parameters have been calculated.The Hammett equation applies very well to the saponification of 3'- and 4'-substituted biphenyl-4-carboxylates with ?-constants evaluated by the FMMF method.The effect of 2'-substituents is understandable in terms of ?-electron steric effects.
- Ananthakrishnanadar, Ponnambalanad.,Kannan, Nagarathnam
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