- Sensitized Two-NIR-Photon Z→E Isomerization of a Visible-Light-Addressable Bistable Azobenzene Derivative
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Two-NIR-photon-triggered Z→E isomerization of an azobenzene was accomplished by covalently linking a two-photon-harvesting triarylamine antenna to a thermally stable ortho-fluorinated azobenzene derivative. The obtained photoswitch is fully addressable wi
- Moreno, Javier,Gerecke, Mario,Grubert, Lutz,Kovalenko, Sergey A.,Hecht, Stefan
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Read Online
- Active ester functionalized azobenzenes as versatile building blocks
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Azobenzenes are important molecular switches that can still be difficult to functionalize selectively. A high yielding Pd-catalyzed cross-coupling method under mild conditions for the introduction of NHS esters to azobenzenes and diazocines has been established. Yields were consistently high with very few exceptions. The NHS functionalized azobenzenes react with primary amines quantitatively. These amines are ubiquitous in biological systems and in material science.
- Schultzke, Sven,Staubitz, Anne,Walther, Melanie
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supporting information
(2021/07/12)
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- Chemical tuning of photoswitchable azobenzenes: A photopharmacological case study using nicotinic transmission
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We have developed photochromic probes for the nicotinic acetylcholine receptor that exploit the unique chemical properties of the tetrafluoroazobenzene (4FAB) scaffold. Ultraviolet light switching and rapid thermal relaxation of the metastable cis configu
- Sansalone, Lorenzo,Zhao, Jun,Richers, Matthew T.,Ellis-Davies, Graham C.R.
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supporting information
p. 2812 - 2821
(2019/12/11)
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- 4 - Bromo - 2, 6 - difluoro aniline synthesis method
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The invention belongs to the field of organic synthetic technology, in particular to a 4 - bromo - 2, 6 - difluoro aniline synthesis method, 2, 6 - difluoro aniline with hydrobromic acid in the presence of hydrogen peroxide produced by the reaction of 4 -
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Paragraph 0022; 0023; 00245; 0005; 00026; 0027; 0028; 0029
(2019/05/15)
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- Modulating Guest Uptake in Core–Shell MOFs with Visible Light
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A two-component core–shell UiO-68 type metal–organic framework (MOF) with a nonfunctionalized interior for efficient guest uptake and storage and a thin light-responsive outer shell was prepared by initial solvothermal MOF synthesis followed by solvent-as
- Mutruc, Dragos,Goulet-Hanssens, Alexis,Fairman, Sam,Wahl, Sebastian,Zimathies, Annett,Knie, Christopher,Hecht, Stefan
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supporting information
p. 12862 - 12867
(2019/08/08)
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- Reversible Stereoselective Folding/Unfolding Fueled by the Interplay of Photoisomerism and Hydrogen Bonding
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A linear molecular architecture equipped with complementary three-fold hydrogen-bonding units embedded with a photoswitchable trans-tetrafluoroazobenzene moiety was synthesized. The transto cis photoisomerism of the azobenzene unit induced drastic changes
- Opie, Christopher R.,Kumagai, Naoya,Shibasaki, Masakatsu
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supporting information
p. 3349 - 3353
(2017/03/17)
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- Photosensitive chiral self-assembling materials: Significant effects of small lateral substituents
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Novel azobenzene-based photosensitive mesogens with lactate chiral units were synthesized. In order to modify the rate of the thermal Z-E isomerization of these compounds, small lateral substituents were introduced into their core in the proximity of the azo group. The influence of lateral substitution on the kinetics of the Z-E isomerization, mesomorphic behaviour, and UV-Vis absorption spectra was studied. It was found that the position of the substituents in the azobenzene core significantly affects the rate of their thermal isomerization. The stability of Z-isomers of several studied compounds is comparable to that of compounds with complex molecular structures designed for optical data storage. Although lateral substitution influences the breadth/length ratio of the core, liquid-crystalline properties of the studied materials have been preserved.
- Cigl, Martin,Bubnov, Alexej,Ka?par, Miroslav,Hampl, Franti?ek,Hamplová, Věra,Pacherová, Oliva,Svoboda, Ji?í
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supporting information
p. 5326 - 5333
(2016/07/06)
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- Development of highly potent phosphodiesterase 10A (PDE10A) inhibitors: Synthesis and in vitro evaluation of 1,8-dipyridinyl- and 1-pyridinyl-substituted imidazo[1,5-a ]quinoxalines
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Herein we report the synthesis of fluorinated inhibitors of phosphodiesterase 10A (PDE10A) which can be used potentially as lead structure for the development of a 18F-labeled PDE10A imaging agent for positron emission tomography. The use of or
- Wagner, Sally,Scheunemann, Matthias,Dipper, Karolin,Egerland, Ute,Hoefgen, Norbert,Steinbach, J?rg,Brust, Peter
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- 4-HETEROARYL SUBSTITUTED BENZOIC ACID COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF
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The present invention relates to compounds according to Formula I (Formula I), and pharmaceutically acceptable salts or solvates thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or conditions.
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Page/Page column 79
(2014/03/22)
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- O -fluoroazobenzenes as readily synthesized photoswitches offering nearly quantitative two-way isomerization with visible light
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Azobenzene functionalized with ortho-fluorine atoms has a lower energy of the n-orbital of the Z-isomer, resulting in a separation of the E and Z isomers' n→π* absorption bands. Introducing para-substituents allows for further tuning of the absorption spe
- Bleger, David,Schwarz, Jutta,Brouwer, Albert M.,Hecht, Stefan
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supporting information
p. 20597 - 20600
(2013/02/22)
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- BICYCLIC INHIBITORS OF ALK
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The present invention relates to compounds of formula (1) or pharmaceutical acceptable salts, wherein R1, X, Y, Z, A, B, G1, and n are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as ALK and methods of treating diseases such as cancer.
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Page/Page column 107
(2012/08/07)
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- BICYCLIC CARBOXAMIDE INHIBITORS OF KINASES
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Compounds of formula (I) or pharmaceutical acceptable salts are provided, wherein X1~X5, R1~R3, A, B, Z and n are defined in the description. And compositions containing said compounds, and the uses for inhibitors of kinases such as ALK, and the uses for treating cancer thereof are provided.
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Page/Page column 70-71
(2012/08/07)
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- Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)- 3,5-difluorobenzoylimino]-thiazol-3-ylmethyl} Ester (Lu AA47070): A phosphonooxymethylene prodrug of a potent and selective hA2A receptor antagonist
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The discovery and structure-activity relationship of a series of hA 2A receptor antagonists is described. Compound 28 was selected from the series as a potent and selective compound and was shown to be efficacious in an in vivo model of Parkinson's disease. It had acceptableADME properties; however, the low intrinsic solubility of this compound was limiting for its developability, because the oral bioavailability from dosing in suspension was significantly lower than the oral bioavailability from solution dosage. As a consequence, prodrugs of 28 were prepared with dramatically increased aqueous solubility. The prodrugs efficiently delivered 28 into systemic circulation, with no detectable levels of prodrug in plasma samples. From this investigation, we selected 32 (Lu AA47070), a phosphonooxymethylene prodrug of 28, as a drug candidate.
- Sams, Anette G.,Mikkelsen, Gitte K.,Larsen, Mogens,Langg?rd, Morten,Howell?, Mark E.,Schr?der, Tenna J.,Brennum, Lise T.,Torup, Lars,J?rgensen, Erling B.,Bundgaard, Christoffer,Kreilg?rd, Mads,Bang-Andersen, Benny
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experimental part
p. 751 - 764
(2011/04/18)
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- Synthesis of novel phenoxyimine ligands containing a 2,6-difluoro-4- styrylaniline
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An efficient synthesis of novel phenoxyimine ligands containing a difluorovinylbiphenyl group was based on the Suzuki coupling coupling of 4-bromo-2,6-difluoroaniline with 4-styrylboronic acid followed by a condensation reaction with various arylaldehydes
- Liu, Bin,Li, Qian,Yu, Mingxin,Liang, Jiaojiao,Fan, Hong,Li, Bogeng
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scheme or table
p. 151 - 153
(2011/07/31)
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- HIV INHIBITING 1,2,4-TRIAZIN-6-ONE DERIVATIVES
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The present invention relates to HIV replication inhibitors of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein ring A and ring B represent phenyl, pyridyl, pyridaz
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Page/Page column 54
(2008/06/13)
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- Liquid-crystalline medium
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A liquid-crystalline medium based on a mixture of polar compounds of positive dielectric anisotropy, which comprises one or more compounds of the formula I where R1, A1, A2, Z1, Z2, L1, Ls
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- The electrophilic substitution of some 2,4- and 2,6- dihaloacetanilides
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The orientation of electrophilic substitution of some 2,4- and 2,6-dihaloacetanilides has been examined by NMR methods. Mixed acid nitration of 2,6-dichloro and 2-chloro-6-methylacetanilides gave predominantly the 3-nitro derivatives.
- Hanson, James R.,Saberi, Hamid
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p. 699 - 701
(2007/10/03)
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- 1,3-dioxane derivative and liquid crystal compositions containing it
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A 1,3-dioxane derivative and a liquid crystal composition containing it as expressed by the general formula STR1 (where R is a straight chain alkyl group of carbon number 1 to 10, A is a single bond or --CH2 CH2 -- group, n is 0 or 1, and the cyclohexane ring and 1,3-dioxane ring are respectively in trans form is disclosed.) The 1,3-dioxane derivative represented by general formula (I) has a very large dielectric anisotropy and a small birefringence. Liquid crystal compositions containing (I) can be driven at low voltage and will provide a liquid crystal display apparatus with a wide visual angle.
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- Pyrimidine derivatives and liquid crystal compositions including same
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2-phenyl-5-(4'-trans-cyclohexyl) phenyl pyrimidine derivatives represented by the general formula: STR1 wherein R is a straight chain alkyl group having 1 to 10 carbon atoms; X is CN or F; Y is F or H; Z is F or H; and when X is F, at least one of Y and Z is H; and the cyclohexane ring is a trans isomer, exhibiting a nematic phase and having a high nematic phase-isotropic liquid phase transition temperature (N-I Point) and large positive dielectric constant anisotropy (Δε). The pyrimidine derivatives may be included in liquid crystal compositions for improved display devices having a wide temperature range, including a high N-I point, a low threshold voltage and a low driving voltage.
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- Pyrimidine derivatives
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2-(3',5'-difluoro-4'-cyanophenyl)pyrimidine derivatives represented by the general formula: STR1 wherein R is a straight chain alkyl having 1 to 10 carbon atoms, n is 0 or 1, the cyclohexane ring is the trans isomer, exhibiting the nematic phase and havin
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- The Synthesis and Transition Temperatures of Some Fluoro-Substituted 4-Cyanophenyl and 4-Cyanobiphenyl-4'-yl 4-Pentyl- and 4-Butoxy-Benzoates
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A series of 4-cyanophenyl 4-X-benzoates and a series of 4-cyanobiphenyl-4'-yl 4-X-benzoates (X= pentyl, butoxy) have been prepared without fluoro-substitution and with mono-fluoro to tetra-fluoro-substitution; all possible combinations of substitution patterns at the positions ortho- to the cyano group and ortho- to the carboxylate group have been obtained in an attempt to determine the structural features which are responsible for some members of these series showing very large positive values of dielectric anisotropy.The synthesis of novel precursors required for the preparation of these esters is described and the melting points and transition temperatures of the esters are discussed and an explanation is provided for the variation of Tn-1 values with position and extent of fluoro-substitution. - Keywords: Fluoro-substitution, phenyl and biphenyl benzoates, terminal cyano namatogens.
- Gray, G. W.,Hird, M.,Lacey, D.,Toyne, K. J.
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p. 165 - 190
(2007/10/02)
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- Pyrimidine derivatives
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Pyrimidine derivatives represented by the general formula: STR1 wherein R is a straight chain alkyl group having from 1 to 12 carbon atoms or an alkoxy group having from 1 to 12 carbon atoms. The pyrimidine derivatives are added to nematic liquid crystal
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- IMIDAZOLETHIOL DOPAMINE-BETA-HYDROXYLASE INHIBITORS
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Potent dopamine-β-hydroxylase inhibitors having the Formula: STR1 which are useful to inhibit dopamine-β-hydroxylase activity, pharmaceutical compositions including these inhibitors, and methods of using these inhibitors to inhibit dopamine-β-hydroxylase
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- Repartitioning Agents: 5--anthranilonitrile and Related Phenethanolamines; Agents for Promoting Growth, Increasing Muscle Accretion and Reducing Fat Deposition in Meat-producing Animals
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A series of phenethanolamines related to clenbuterol was prepared and examined in mice for growth-promoting and fat-reducing activities.Several analogs were equipotent to clenbuterol.In chickens, 5-anthranilonitrile appeared to be more potent than clenbuterol with recpect to "repartitioning" activity, that is, the ability to redirect food energy from fat formation to muscle accretion.Based on this potency and low residue levels in edible tissues, this compound is in advanced stages of evaluation for commercial use in meat animals.
- Asato, Goro,Baker, Pamela K.,Bass, Roy T.,Bentley, T. James,Chari, Sarangan,et al.
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p. 2883 - 2888
(2007/10/02)
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