- Impact of substitution pattern and chain length on the thermotropic properties of alkoxy-substituted triphenyl-tristriazolotriazines
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Tristriazolotriazines (TTTs) with a threefold alkoxyphenyl substitution were prepared and studied by DSC, polarized optical microscopy (POM) and X-ray scattering. Six pentyloxy chains are sufficient to induce liquid-crystalline behavior in these star-shap
- Detert, Heiner,Glang, Stefan,Haspel, Tobias,Lehmann, Matthias,Limbach, Daniel,Rieth, Thorsten,Schupp, Niklas,Sperner, Marcel,Tober, Natalie,Wicker, Philipp
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supporting information
(2021/06/14)
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- Btk INHIBITORS WITH IMPROVED DUAL SELECTIVITY
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Disclosed herein is a tri-substituted phenyl Btk inhibitors with improved dual selectivity, a method and a composition for inhibiting Btk and treating disease associated with undesirable Btk activity (Btk-related diseases).
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Paragraph 0230-0232
(2019/03/05)
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- Total Synthesis of Gramistilbenoids A, B, and C
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Stilbenes are biologically active metabolites of plants that have the potential to attenuate a broad range of human diseases. Gramistilbenoids are a class of natural products with a stilbene skeleton, isolated from the bamboo orchid (Arundina graminifolia), and with significant cytotoxicity against cancer cell lines (NB4, A549, SHSY5Y, PC3, and MCF7). These are the first identified naturally occurring diphenylethylenes to possess a hydroxyethyl unit. However, some of these compounds are not abundant in nature, and thus, their synthesis is advantageous. This paper reports the first synthesis of gramistilbenoids A (1), B (2), and C (3), with overall yields of 10, 2, and 8% respectively. These natural products were synthesized using key reactions, such as Horner-Wadsworth-Emmons olefination, Stille coupling, and hydroboration-oxidation.
- Harmalkar, Dipesh S.,Lu, Qili,Lee, Kyeong
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supporting information
p. 798 - 805
(2018/05/07)
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- Synthesis and NMR analysis of a conformationally controlled β-Turn Mimetic Torsion Balance
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The molecular torsion balance concept was applied to a new conformationally controlled scaffold and synthesized to accurately evaluate pairwise amino acid interactions in an antiparallel β-sheet motif. The scaffold's core design combines (ortho-tolyl)amide and o,o,o′-trisubstituted biphenyl structural units to provide a geometry better-suited for intramolecular hydrogen bonding. Like the dibenzodiazocine hinge of the traditional torsion balance, the (ortho-tolyl)amide unit offers restricted rotation around an N-aryl bond. The resulting two-state folding model is a powerful template for measuring hydrogen bond stability between two competing sequences. The aim of this study was to improve the alignment between the amino acid sequences attached to the upper and lower aromatic rings in order to promote hydrogen bond formation at the correct distance and antiparallel orientation. Bromine substituents were introduced ortho to the upper side chains and compared to a control to test our hypothesis. Hydrogen bond formation has been identified between the NH amide proton of the upper side chain (proton donor) and glycine acetamide of the lower side chain (proton acceptor).
- Lypson, Alyssa B.,Wilcox, Craig S.
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p. 898 - 909
(2017/11/04)
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- Heterocyclic compound and application thereof
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The invention belongs to the field of medical chemistry, and relates to a heterocyclic compound and application thereof. Concretely, the invention provides a compound as shown in a formula I, or an isomer, pharmaceutically acceptable salts, and a solvate
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Paragraph 0092; 0093
(2017/08/29)
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- Ruthenium-Catalyzed Hydroarylation and One-Pot Twofold Unsymmetrical C?H Functionalization of Arenes
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A methyl phenyl sulfoximine (MPS) is used as a directing group in the ruthenium-catalyzed intramolecular hydroarylation of alkene-tethered benzoic acid derivatives to afford dihydrobenzofurans and indolines in good to excellent yields. A one-pot, unsymmetrical, twofold C?H functionalization involving intramolecular C?C and intermolecular C?C/C?N bond formations is successfully demonstrated by using a single set of catalytic reaction conditions, which is unprecedented thus far. A novel isoquinolone-bearing dihydrobenzofuran is constructed through an unsymmetrical twofold C?H functionalization.
- Ghosh, Koushik,Ramesh, E.,Rit, Raja K.,Sahoo, Akhila K.
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supporting information
p. 7821 - 7825
(2016/07/07)
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- LIPIDS AND LIPID COMPOSITIONS FOR THE DELIVERY OF ACTIVE AGENTS
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This invention provides for a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1–R4, L and X are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.
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Page/Page column 124
(2014/09/29)
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- New meso-substituted trans-A2B2 di(4-pyridyl) porphyrins as building blocks for metal-mediated self-assembling of 4 + 4 Re(i)-porphyrin metallacycles
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The reaction between 5-(4-pyridyl)dipyrrylmethane and aromatic aldehydes affords meso-arylsubstituted trans-A2B2 di(4-pyridyl)porphyrins which are key building blocks in the metal-mediated self-assembling of supramolecular structures
- Boccalon, Mariangela,Iengo, Elisabetta,Tecilla, Paolo
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p. 4056 - 4067
(2013/07/05)
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- SPIROCHROMANON DERIVATIVES
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The invention relates to a compound of a general formula (I): wherein Ar1 represents a group formed from an aromatic ring selected from a group consisting of benzene, pyrazole, isoxazole, pyridine, indole, 1H-indazole, 1H-furo[2,3-c]pyrazole, 1H-thieno[2,3-c]pyrazole, benzimidazole, 1,2-benzisoxazole, imidazo[1,2-a]pyridine, imidazo[1,5-a]pyridine and 1H-pyrazolo[3,4-b]pyridine, having Ar2, and optionally having one or two or more substituents selected from R3; R1 and R2 each independently represent a hydrogen atom, a halogen atom, a cyano group, a C2-C6 alkenyl group, a C1-C6 alkoxy group, a C2-C7 alkanoyl group, a C2-C7 alkoxycarbonyl group, an aralkyloxycarbonyl group, a carbamoyl-C1-C6 alkoxy group, a carboxy-C2-C6 alkenyl group, or a group of -Q1-N(Ra)-Q2-Rb; or a C1-C6 alkyl group optionally having a substituent; or an aryl or heterocyclic group optionally having a substituent; or a C1-C6 alkyl group or a C2-C6 alkenyl group having the aryl or heterocyclic group; T and U each independently represent a nitrogen atom or a methine group; and V represents an oxygen atom or a sulfur atom. The compound of the invention is useful as therapeutical agents for various ACC-related diseases.
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Page/Page column 136
(2008/12/07)
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- A new family of biisoquinoline chelates
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Four 8,8′-diaryl-substituted 3,3′-biisoquinoline ligands have been synthesized and characterized. The key feature of this new family of chelates is their endotopic but sterically non-hindering nature. All four ligands were made from a common 8-bromoisoquinolin-3-ol precursor; between three and twelve synthetic steps were necessary to obtain the products. The reported synthetic procedures allow for gram-scale production of these biisoquinolines. Wiley-VCH Verlag GmbH & Co. KGaA, 2007.
- Durola, Fabien,Hanss, David,Roesel, Pirmin,Sauvage, Jean-Pierre,Wenger, Oliver S.
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p. 125 - 135
(2007/10/03)
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- Concave pyridines for bifunctional acid-base catalysis
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Two bifunctional concave acid-base catalysts, 1 and 2, have been synthesized starting from 2,6-dibromopyridine (9) and 2,6-bis(ω- alkenyloxy)phenylboronic acids 8 and 10 which end up as bridgeheads in final bimacrocycles 1 and 2. One bridgehead contained
- Liebig, Timo,Abbass, Michael,Luening, Ulrich
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p. 972 - 980
(2008/02/13)
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- Total synthesis of (+)-machaeriol D with a key regio- and stereoselective SN2′ reaction
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(Chemical Equation Presented) A general strategy for the synthesis of hexahydrodibenzopyrans (HHDBPs) is illustrated in the enantioselective total synthesis of (+)-machaeriol D. In the key step, an SN2′ reaction of an aryl cyanocuprate with a s
- Wang, Qiaoling,Huang, Qinggang,Chen, Bo,Lu, Jiangping,Wang, Hui,She, Xuegong,Pan, Xinfu
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p. 3651 - 3653
(2008/03/12)
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- Cleavable surfactants and methods of use thereof
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Cleavable compositions and methods of use especially in MALDI MS analysis of hydrophobic proteins.
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- Total synthesis of the turrianes and evaluation of their DNA-cleaving properties
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The first total synthesis of three naturally occurring cyclophane derivatives belonging to the turriane family of natural products is described. Their sterically hindered biaryl entity is formed by reaction of the Grignard reagent derived from aryl bromide 10 with the oxazoline derivative 18, and the macrocyclic tether of the targets is efficiently forged by ring closing metathesis. While conventional RCM catalyzed by the ruthenium-carbene complexes 33 or 34 invariably leads to the formation of mixtures of both stereoisomers with the undesirable (E)-alkene prevailing, ring closing alkyne metathesis (RCAM) followed by Lindlar reduction of the resulting cycloalkynes 37 and 38 opens a convenient and stereoselective entry into this class of compounds. RCAM can either be accomplished by using the tungsten alkylidyne complex [(tBuO)3W≡CCMe3] or by means of a catalyst formed in situ from [Mo(CO)6] and para-trifluoromethylphenol. The latter method is significantly accelerated when carried out under microwave heating. Furthermore, the judicious choice of the protecting groups for the phenolic-OH functions turned out to be crucial. PMB-ethers were found to be compatible with the diverse reaction conditions en route to 3-5; their cleavage, however, had to be carried out under carefully optimized conditions to minimize competing O-C PMB migration. Turrianes 3-5 are shown to be potent DNA cleaving agents under oxidative conditions when administered in the presence of copper ions.
- Fuerstner, Alois,Stelzer, Frank,Rumbo, Antonio,Krause, Helga
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p. 1856 - 1871
(2007/10/03)
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- Synthesis of the racemate of the stereoisomer at C-6a of BE-40644, a bioactive metabolite of Actinoplanes sp. with a sesquiterpene-substituted p-benzoquinone structure.
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BE-40644 is a tetracyclic metabolite of Actinoplanes sp. A 40644 possessing a sesquiterpene-substituted p-benzoquinone structure with cis-fused B/C ring stereochemistry that inhibits the human thioredoxin system as the well as the growth of several cancer cell lines. Its B/C trans-fused stereoisomer at C-6a was synthesized as a racemate starting from geranylacetone and 3,5-dihydroxybenzoic acid.
- Tsujimori,Mori
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p. 167 - 171
(2007/10/03)
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- A Facile Synthetic Route to a Third-Generation Dendrimer with Generation-Specific Functional Aryl Bromides
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(Formula Presented) The synthesis of three third-generation dendrimers that selectively carry one aryl bromide functional group in the first, second, or third generation, respectively, is described. These functions, regardless of their location, can be ch
- Bo, Zhishan,Schaefer, Andreas,Franke, Peter,Schlueter, A. Dieter
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p. 1645 - 1648
(2007/10/03)
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- Total synthesis of enantiomerically pure (-)-Balanol
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The total synthesis of enantiomerically pure (-)-Balanol (1), using tri-O-acetyl-D-glucal as a chiral template for the central azepane fragment is described.
- Barbier, Pierre,Stadlwieser, Josef
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p. 530 - 532
(2007/10/03)
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