- Total Synthesis of Viridin and Viridiol
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The asymmetric total synthesis of (-)-viridin and (-)-viridiol, antifungal metabolites, was achieved in 17 and 18 steps from a commercially available starting material. An intramolecular [3+2] cycloaddition was applied to an easily available l-ribose derivative in order to construct the highly substituted D ring containing the key chiral cis-triol fragment. Co-catalyzed metal-hydride H atom transfer (MHAT) radical cyclization was utilized to form the C-ring and the all-carbon quaternary center at C-10. This convergent strategy provides a scalable approach to prepare viridin and viridiol for biological studies.
- Ji, Yang,Xin, Zhengyuan,He, Haibing,Gao, Shuanhu
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- FUSED PYRAZOLE AND IMIDAZOLE BASED COMPOUNDS AND USE THEREOF AS GLI1 INHIBITORS
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The present invention is directed to a composition and a method for use thereof, such as for the treatment and prevention of a neurological disorder or cancer in a subject.
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Paragraph 00197; 00205
(2021/11/20)
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- S1P1 AGONIST AND APPLICATION THEREOF
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The present invention relates to a class of tricyclic compounds and an application thereof as a sphingosine 1-phosphate type 1 (S1P1) receptor agonist. The invention specifically relates to a compound represented by formula (II), and a tautomer and pharmaceutically acceptable salt of same.
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Paragraph 0608-0611
(2021/10/02)
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- Enantioselective Synthesis of Chiral Indane Derivatives by Rhodium-Catalyzed Addition of Arylboron Reagents to Substituted Indenes
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Rhodium-catalyzed asymmetric addition of arylboron reagents to indene derivatives proceeded to give 2-arylindanes in good yields with high enantioselectivity. Deuterium-labeling experiments indicated that the present reaction involved a 1,4-Rh shift from an initially formed benzylrhodium to an arylrhodium intermediate before protonation leading to the corresponding addition product. The asymmetric addition was also successful for acenaphthylene, which has a similar skeleton to indene, where it was found that the benzylrhodium intermediate underwent direct protonation without the 1,4-Rh shift.
- Umeda, Moeko,Noguchi, Hikaru,Nishimura, Takahiro
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supporting information
p. 9597 - 9602
(2020/12/21)
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- Aromatic ring-containing compound and application thereof
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The present invention discloses an aromatic ring-containing compound and an application thereof, and provides an aromatic ring-containing compound represented by formula I, and a pharmaceutically acceptable salt, a hydrate, a solvate, a metabolite, a ster
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Paragraph 0112-0116
(2019/10/01)
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- Asymmetric Magnesium-Catalyzed Hydroboration by Metal-Ligand Cooperative Catalysis
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Asymmetric catalysis with readily available, cheap, and non-toxic alkaline earth metal catalysts represents a sustainable alternative to conventional synthesis methodologies. In this context, we describe the development of a first MgII-catalyzed enantioselective hydroboration providing the products with excellent yields and enantioselectivities. NMR spectroscopy studies and DFT calculations provide insights into the reaction mechanism and the origin of the enantioselectivity which can be explained by a metal-ligand cooperative catalysis pathway involving a non-innocent ligand.
- Falconnet, Alban,Magre, Marc,Maity, Bholanath,Cavallo, Luigi,Rueping, Magnus
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supporting information
p. 17567 - 17571
(2019/11/13)
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- Metallocenes and catalyst compositions derived therefrom
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This invention relates to a novel group 2, 3 or 4 transition metal metallocene catalyst compound that is asymmetric having two non-identical indenyl ligands with substitution at R2 having a branched or unbranched C1-C20 alkyl group substituted with a cyclic group or a cyclic group, R8 is an alkyl group and R4 and R10 are substituted phenyl groups.
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- Metallocenes and Catalyst Compositions Derived Tehrefrom
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This invention relates to a novel group 2, 3 or 4 transition metal metallocene catalyst compound that is asymmetric having two non-identical indenyl ligands with substitution at R2 having a branched or unbranched C1-C20 alkyl group substituted with a cyclic group or a cyclic group, R8 is an alkyl group and R4 and R10 are substituted phenyl groups.
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- BRIDGED BIS(INDENYL) TRANSITIONAL METAL COMPLEXES, PRODUCTION, AND USE THEREOF
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The invention relates to a novel group bridged metallocene transition metal complexes, wherein the complex includes at least one indenyl ligand substituted at the 4- position with a phenyl group, the 4-phenyl group being preferably substituted at the 3 ', 4', and 5' positions with particular combinations of substituents, particularly wherein the 4'- substituent is a group of the formula (XR'n)-, wherein X is a Group 14-17 heteroatom having an atomic weight of 13 to 79 and R' is one of a hydrogen atom, halogen atom, a C1-C10 alkyl group, or a C6-C10 aryl group and n is 0, 1, 2, or 3. Catalyst systems including the transition metal complex, polymerization processes using the transition metal complex, and polymers made using the transition metal complex are also described.
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- SELECTIVE HETEROCYCLIC SPHINGOSINE 1 PHOSPHATE RECEPTOR MODULATORS
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Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds is provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.
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Paragraph 0260; 0261
(2015/11/18)
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- Construction of polyaromatics via photocyclization of 2-(fur-3-yl) ethenylarenes, using a 3-furyl group as an isopropenyl equivalent synthon
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The construction of different types of substituted arenes was demonstrated through the photocyclization of 2-(fur-3-yl)ethenylarenes using a 3-furyl group as an isopropenyl equivalent synthon in the photocyclization reaction. The furan portion of the photocyclization intermediate could be fragmented via a base-induced elimination reaction to yield a series of substituted polyaromatics, including naphthalene, benzofuran, benzothiophene, phenanthrene, phenalene, acenaphthene, and triphenylene. Using different reagents, this method made it possible to introduce methyl or 2-hydroxyethyl groups as substituents at specific positions in these arenes.
- Chen, Ying-Zhe,Ni, Ching-Wen,Teng, Fu-Lin,Ding, Yi-Shun,Lee, Tunng-Hsien,Ho, Jinn-Hsuan
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p. 1748 - 1762
(2014/03/21)
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- Palladium nanoparticles in Suzuki cross-couplings: Tapping into the potential of tris-imidazolium salts for nanoparticle stabilization
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Inspired by the proclivity of various palladium sources to form nanoparticles in imidazolium-based ionic liquids, we now report that tris-imidazolium salts bearing hexadecyl chains and a bridging mesitylene moiety are potent stabilizers of palladium nanoparticles efficiently prepared via a Chaudret-type hydrogenation of the bis(dibenzylideneacetone)palladium(0). The palladium nanoparticles have been isolated in pure form and characterized by 1H nuclear magnetic resonance, transmission electron microscopy, electron diffraction and dynamic light scattering. The new materials proved effective in Suzuki cross-coupling at a loading of 0.2% palladium. Thus, using a tris-imidazolium iodide-palladium material, a series of biaryl products has been prepared starting from aryl bromides and some activated chlorides. The possibility that this catalytic activity might be due to the formation of palladium N-heterocyclic carbenes has been addressed through solid state 13C NMR and the synthesis of an imidazolium analogue in which the acidic 2-H was replaced with a methyl group. Copyright
- Planellas, Marc,Pleixats, Roser,Shafir, Alexandr
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p. 651 - 662
(2012/05/04)
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- NOVEL 3-HYDROXY-5-ARYLISOXAZOLE DERIVATIVE
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[Problem] To provide a GPR40 activating agent having, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the salt or the compound, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of solving the problem] A compound of Formula (I): (where p is 0 to 4; j is 0 to 3; k is 0 to 2; a ring A is a specific cyclic group; a ring B is a benzene ring, a pyridine ring, or a pyrimidine ring; X is —CH2—, O, —S(O)i— (i is 0 to 2), or —NR7—; R1 to R6 are specific groups), a salt of the compound, or a solvate of the salt or the compound.
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Page/Page column 61
(2012/09/10)
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- SPHINGOSINE 1 PHOSPHATE RECEPTOR MODULATORS AND METHODS OF CHIRAL SYNTHESIS
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Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds is provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.
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Page/Page column 78
(2011/06/16)
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- 1,2,3-trisubstituted indanes by highly diastereoselective palladium-catalyzed oxyarylation of indenes with arylboronic acids and nitroxides
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Chemecal quation presented Excellent stereoselectivity is obtained in the synthesis of biologically interesting 1,2,3-trisubstituted indanes B by the reaction of readily prepared 3-substituted indenes A with commercially available arylboronic acids by using various TEMPO derivatives as external oxidants and Pd(OAc)2 as a catalyst. The anti,anti isomers are formed and reactions occur stereospecifically under mild conditions.
- Kirchberg, Sylvia,Froehlich, Roland,Studer, Armido
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supporting information; experimental part
p. 6877 - 6880
(2010/12/19)
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- Pyrethrinoid esters carrying an indanyl nucleus and their use as pesticides
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Pyrenthrinoid esters with an indenyl nucleus having the following structural formula STR1 wherein the substituents are herein defined, have been shown to be useful as pesticides and in pesticidal compositions.
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- Synthesis of Biological Markers in Fossil Fuels. 2. Synthesis and 13C NMR Studies of Substituted Indans and Tetralins
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Unambiguous syntheses of all possible methyl, ethyl, n-propyl, and n-butyl derivatives of indan and tetralin were developed using the Kumada coupling procedure involving the reaction of aryl or vinyl halides with Grignard reagents in the presence of nickel(II) chloride.An analysis of the 13C NMR spectra of these compounds was also completed.
- Adamczyk, Maciej,Watt, David S.,Netzel, Daniel A.
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p. 4226 - 4237
(2007/10/02)
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