- 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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- Ring-fused compound, preparation method thereof and application of compound
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The invention relates to a ring-fused compound or pharmaceutically acceptable salt thereof, ester, a steric isomer, a tautomer, a polymorphic substance, a solvate, a hydrate, a metabolite or prodrug or mixture of the materials, a medicine composition and medicine box product comprising the compound, a preparation method of the compound and an application of the compound to preparation of medicinesfor preventing or treating PD-1/PD-L1 related diseases.
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Paragraph 0160; 0161; 0164; 0165
(2019/05/02)
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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 0112-0114; 0117; 0118
(2019/10/01)
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- IMMUNOMODULATOR COMPOUNDS
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Compounds are provided that are useful as immunomodulators. The compounds have the following Formula (II): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, R2a, R2b, R2c, R3, R4, R5, R6a, R6b, m and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
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Paragraph 0192; 0193
(2018/02/28)
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- HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS
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Disclosed are compounds of Formula (I′), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds inhibit PD-1/PD-L1 interaction and are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.
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Paragraph 0542-0543
(2018/07/15)
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- Copper-Catalyzed Enantioselective Domino Arylation/Semipinacol Rearrangement of Allylic Alcohols with Diaryliodonium Salts
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A copper-catalyzed enantioselective arylative semipinacol rearrangement of allylic alcohols was developed. In the presence of a catalytic amount of an in situ generated chiral copper-bisoxazoline complex, reaction of allylic alcohols with diaryliodonium salts afforded spirocycloalkanones in high yields with high diastereo- and enantioselectivities. A two-point binding model engaging the carbon–carbon double bond and the proximal hydroxyl group was proposed to be responsible for the highly efficient chirality transfer.
- Wu, Hua,Wang, Qian,Zhu, Jieping
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supporting information
p. 13037 - 13041
(2017/09/26)
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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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supporting information; experimental part
p. 651 - 662
(2012/05/04)
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- Water-soluble palladium nanoparticles: Click synthesis and applications as a recyclable catalyst in Suzuki cross-couplings in aqueous media
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A new PEG-tagged material, which was prepared by a threefold copper-catalyzed [3+2] cycloaddition (click chemistry), was found to act as an efficient stabilizer for palladium nanoparticles. The newly formed material proved to be active asa recyclable catalyst in Suzuki coupling the presence of polyether chains allowed for the catalytic runs to be conducted in aqueous media.
- Mejias, Nereida,Pleixats, Roser,Shafir, Alexandr,Medio-Simon, Mercedes,Asensio, Gregorio
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supporting information; experimental part
p. 5090 - 5099
(2010/10/21)
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- 4-Phenyl-2-indanyl esters of 1R,cis-3-(2-halo-3,3,3-trifluoropropenyl)-2,2-dimethylcyclopropanecarboxylic acid
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Insecticidal 4-phenyl-2-indanyl 1R,cis-3-(2-halo-3,3,3-trifluoro-1-propenyl)-2,2-dimethylcyclopropanecarboxylates having a racemic or optically active indanyl moiety, methods of preparation and use, and efficacy data against representative insect species are disclosed and exemplified.
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- Insecticidal pyrethroid enantiomer pair
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An insecticidal enantiomer pair consisting essentially of a substantially equimolar mixture of S-4-phenyl-2-indanyl 1R, cis-3-(2-chloro-3,3,3-trifluoro-1-propenyl)-2,2-dimethylcyclopropanecarboxylate and R-4-phenyl-2-indanyl 1S,cis-3-(2-chloro-3,3,3-trifluoro-1-propenyl)-2,2-dimethylcyclopropanecarboxylate, its preparation by liquid chromatography, and its utility as an insecticide are described and exemplified.
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- 4-Substituted-2-indanols
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Novel compounds of the formula STR1 are disclosed in which R1 is a phenyl, phenoxy, phenylthio, benzyl or heterocyclic radical which may be substituted, and R2 is hydrogen. The compounds are intermediates of cyclopropanecarboxylate and related insecticides.
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- 4-Substituted-2-indanol insecticidal ester derivatives
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Novel compounds of the formula STR1 are disclosed in which R1 is a phenyl, phenoxy, phenylthio, benzyl or heterocyclic radical which may be substituted, and R2 is hydrogen, a substituted-vinylcyclopropanecarbonyl group, a tetramethylcyclopropanecarbonyl group, or a 1-(substituted-phenyl)-2-methylpropylcarbonyl group. The compounds wherein R2 is other than hydrogen are insecticides.
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