- Rhodium-Catalyzed Synthesis of Chiral Monohydrosilanes by Intramolecular C?H Functionalization of Dihydrosilanes
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The preparation of chiral monohydrosilanes remains a rarely achieved goal. To this end a Rh-catalyzed desymmetrization of dihydrosilanes by way of intramolecular C(sp2)?H functionalization under simple and mild conditions has now been developed
- Ma, Wenpeng,Liu, Li-Chuan,An, Kun,He, Tao,He, Wei
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supporting information
p. 4245 - 4251
(2020/12/25)
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- Further lead optimization on Bax activators: Design, synthesis and pharmacological evaluation of 2-fluoro-fluorene derivatives for the treatment of breast cancer
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To further pursue potent Bax activators with better safety profiles for the treatment of breast cancer, structural optimization was conducted based on lead compound CYD-4-61 through several strategies, including scaffold hopping on the 2-nitro-fluorene ring, replacement of the nitro group with bioisosteres to avoid potential toxicity, and further optimization on the upper pyridine by exploring diverse alkylamine linkers as a tail or replacing the pyridine with bioisosteric heterocycles. F-containing compound 22d (GL0388) exhibited a good balance between the activity and toxicity, displaying submicromolar activities against a variety of cancer cell lines with 5.8–10.7-fold selectivity of decreased activity to MCF-10A human mammary epithelial cell line. Compound 22d dose-dependently blocked colony formation of breast cancer cells and prevented the migration and invasion of MDA-MB-231 cells. Mechanism of action studies indicate that 22d activated Bax, rendering its insertion into mitochondrial membrane, thereby leading to cytochrome c release from the mitochondria into the cytoplasm, subsequently inducing release of apoptotic biomarkers. Further in vivo efficacy studies of 22d in human breast cancer xenografts arisen from MDA-MB-231 cells demonstrated that this drug candidate significantly suppressed tumor growth, indicating the therapeutic promise of this class of compounds for the treatment of breast cancer as well as the potential for developing F-radiolabeled imaging ligands as anticancer chemical probes.
- Liu, Gang,Kim, Hyejin,Wang, Pingyuan,Fricke, Doerte R.,Chen, Haiying,Wang, Tianzhi,Shen, Qiang,Zhou, Jia
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- Synthesis of Dibenzosiloles through Electrocatalytic Sila-Friedel-Crafts Reaction
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A novel electrocatalyzed method for the preparation of dibenzosiloles was developed through intramolecular C?H/Si?H dehydrogenative coupling strategy starting from biarylhydrosilanes. Both electro-donating and electro-withdrawing substitution groups were tolerated for this transformation, and the desired dibenzosilole products could be obtained in moderate to excellent yields. A sila-Friedel-Crafts reaction mechanism was proposed on the basis of previous literature and our controlled experiments. (Figure presented.).
- Han, Pan,Yin, Mengyun,Li, Haiqiong,Yi, Jundan,Jing, Linhai,Wei, Bangguo
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supporting information
p. 2757 - 2761
(2021/04/16)
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- Palladium-catalyzed relay C–H functionalization to construct novel hybrid-arylcyclophosphorus ligand precursors
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A new relay C–H functionalization of di([1,1′-biphenyl]-2-yl)phosphine oxide to obtain esterified and hydroxylated products with different hypervalent iodines as oxidants under palladium catalysis is disclosed. This reaction provides a more effective and concise strategy for the synthesis of novel structural hybrid-arylcyclophosphorus ligand precursors with a wide range of substrates and good functional group tolerance.
- Bai, Peng-Bo,Wang, Juan,Yang, Shang-Dong
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supporting information
(2021/11/17)
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- Ag-Catalyzed Cyclization of Arylboronic Acids with Elemental Selenium for the Synthesis of Selenaheterocycles
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A general method for the synthesis of five-membered and six-membered selenaheterocycles through Ag-catalyzed C?Se bond-forming reaction is reported. This reaction proceeds via intramolecular cyclization of arylboronic acids with selenium powder. Preliminary mechanism studies demonstrate that this transformation involves a selenium-centred radical intermediate. (Figure presented.).
- Gao, Wen-Xia,Huang, Xiao-Bo,Liu, Miao-Chang,Wu, Hua-Yue,Zhang, Xue,Zhou, Yun-Bing
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supporting information
p. 5639 - 5644
(2020/11/30)
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- Visible-Light-Promoted, Catalyst-Free Gomberg-Bachmann Reaction: Synthesis of Biaryls
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Biaryls were synthesized via a novel visible-light-promoted Gomberg-Bachmann reaction that does not require a photosensitizer or any metal reagents. The formation of an electron donor-acceptor complex between aryl diazonium salts and pyridine allows, under visible-light irradiation, the synthesis of biaryls in moderate-to-high yields.
- Lee, Juyoung,Hong, Boseok,Lee, Anna
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p. 9297 - 9306
(2019/08/12)
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- Condensed fluorene derivative comprising heterocyclic ring
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The present invention relates to a condensed fluorene derivative comprising a heterocyclic ring and, more particularly, to an intermediate product for manufacturing a heterocyclic ring compound which can show excellent luminance and luminous efficiency when used as an organic light emitting material, while exhibiting excellent element characteristics with a long lifespan.COPYRIGHT KIPO 2020
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Paragraph 0397-0403
(2019/12/25)
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- Visible-Light Induced Radical Silylation for the Synthesis of Dibenzosiloles via Dehydrogenative Cyclization
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A visible-light induced radical silylation to dibenzosiloles from biarylhydrosilanes is described. The products were obtained in satisfactory yields under mild and water/air compatible conditions, providing an efficient and practical method for the synthesis of difunctionalized siloles by using a cheap organic dye photocatalyst. The method is tolerated by a wide range of functional groups and has a broad substrate scope. Light/dark experiments and quantum yield measurements provided support for a photocatalytic pathway rather than a chain process. (Figure presented.).
- Yang, Chao,Wang, Jing,Li, Jianhua,Ma, Wenchao,An, Kun,He, Wei,Jiang, Chao
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supporting information
p. 3049 - 3054
(2018/08/06)
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- NOVEL INHIBITORS
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The invention relates to a compound of formula (I): A-B-D-E (I) or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein: A is selected from monocyclic and bicyclic heteroaryl, which may independently substituted by alkyl or amino; B is selected from alkyl, heteroalkyl, alkyl-amino, aryl, heteroaryl, cycloalkyl, heterocyclyl and alkylene, wherein said groups may independently be substituted by alkyl; D is selected from aryl-amino, heteroaryl-amino, cycloalkyl-amino, heterocyclyl, heterocyclyl-amino, urea, thioamide, thiourea, sulfonamide, sulfoximine and sulfamoyl, wherein said aryl, heteroaryl, cycloalkyl and heterocyclyl groups may independently be substituted; and E is selected from aryl, heteroaryl, cycloalkyl, heterocyclyl, wherein said aryl, heteroaryl, cycloalkyl and heterocyclyl groups may independently be substituted. The compounds of formula (I) are inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N- terminal glutamate residues into pyroglutamic acid under liberation of water.
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Page/Page column 183
(2018/10/25)
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- Construction of Chiral Tetraorganosilicons by Tandem Desymmetrization of Silacyclobutanes/Intermolecular Dehydrogenative Silylation
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We report a method to construct chiral tetraorganosilicons by tandem silacyclobutane (SCB) desymmetrization–dehydrogenative silylations. A wide array of dibenzosiloles with stereogenic quaternary silicon centers were obtained in good yields and enantioselectivities up to 93 % ee. Chiral TMS-segphos was found to be a superior ligand in terms of reactivity and enantioselectivity.
- Zhang, Qing-Wei,An, Kun,Liu, Li-Chuan,Zhang, Qi,Guo, Huifang,He, Wei
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supporting information
p. 1125 - 1129
(2017/01/18)
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- Synthetic method for 9,10-benzophenanthrene compound
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The invention discloses a synthetic method for a 9,10-benzophenanthrene compound. The synthetic method comprises the following concrete steps: dissolving a compound as shown in a formula (2) which is described in the specification and another compound as shown in a formula (4) which is described in the specification in N,N-dimethyl formamide under the protection of inert gas; and carrying out a reaction at 120 to 140 DEG C under the action of copper trifluoromethanesulfonate, sodium carbonate and caesium acetate so as to obtain the 9,10-benzophenanthrene compound as shown in a formula (I) which is described in the specification. According to the invention, 2-bromobiphenyl is used as a raw material, diaryl iodate is used as an arylation reagent, bivalent copper is used as a catalyst, and sodium carbonate and caesium acetate are used as mixed base; the synthetic method has the characteristics of usage of easily available raw materials, short reaction time, high yield, etc.; and as a simplest graphene monomer, the synthesized 9,10-benzophenanthrene compound good application prospects in the field of organic photoelectricity.
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Paragraph 0051; 0052; 0053
(2018/01/09)
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- Rhodium-catalyzed intramolecular C-H silylation by silacyclobutanes
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Silacyclobutane was discovered to be an efficient C-H bond silylation reagent. Under the catalysis of RhI/TMS-segphos, silacyclobutane undergoes sequential C-Si/C-H bond activations, affording a series of π-conjugated siloles in high yields and regioselectivities. The catalytic cycle was proposed to involve a rarely documented endocyclic β-hydride elimination of five-membered metallacycles, which after reductive elimination gave rise to a Si-RhI species that is capable of C-H activation. Old reagent, new reactivity: Silacyclobutane was discovered to be an efficient C-H bond silylation reagent under the catalysis of Rh/TMS-segophos. This new reactivity was attributed to a key Si-RhI intermediate formed through a Si-C activation, endocyclic β-H elimination and reductive elimination cascade. A wide array of siloles was obtained in high yields and excellent regioselectivities.
- Zhang, Qing-Wei,An, Kun,Liu, Li-Chuan,Guo, Shuangxi,Jiang, Chenran,Guo, Huifang,He, Wei
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supporting information
p. 6319 - 6323
(2016/05/24)
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- Condensed fluorene derivative comprising heterocyclic ring
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The present invention relates to a condensed fluorene derivative comprising a heterocyclic ring and, more particularly, to an intermediate product for manufacturing a heterocyclic ring compound which can show excellent luminance and luminous efficiency when used as an organic light emitting diode, while having excellent element characteristics with long lifespan. The heterocyclic ring compound of the present invention is represented by chemical formula A and chemical formula B.COPYRIGHT KIPO 2016
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Paragraph 0397-0403
(2016/10/08)
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- 9-Silafluorenes via base-promoted homolytic aromatic substitution (BHAS) - The electron as a catalyst
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Transition-metal-free intramolecular radical silylation of 2-diphenylsilylbiaryls via base-promoted homolytic aromatic substitution (BHAS) to give 9-silafluorenes is reported. 2-Diphenylsilylbiaryls are readily prepared, and cross dehydrogenative silylation occurs with tert-butylhydroperoxide (TBHP) as a cheap stoichiometric oxidant in the presence of a small amount of tetrabutylammonium iodide (TBAI) as an initiator. These cyclizations are catalyzed by the electron.
- Leifert, Dirk,Studer, Armido
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supporting information
p. 386 - 389
(2015/01/30)
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- Novel aromatic compounds for organic light-emitting diode and organic light-emitting diode including the same
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The present invention relates to an organic light emitting compound represented by chemical formula A, and to an organic light emitting device comprising the same. In the chemical formula A, a cyclic group A_1 to A_3, R_1 to R_11, L, n, a structural formula Q, and a structural formula Aandprime; are the same as described in the specification.COPYRIGHT KIPO 2016
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Paragraph 0223-0226; 0464-0469
(2016/10/09)
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- Heterocyclic compound comprising aromatic amine group and organic light-emitting diode including the same
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The present invention relates to a heterocyclic compound comprising an aromatic amine group and an organic light emitting device including the same and, more specifically, to a heterocyclic compound, which has excellent luminance, luminance efficiency, and outstanding long lifespan characteristics when being used as an organic light emitting material. In addition, the present invention further relates to an organic light emitting device including the same.COPYRIGHT KIPO 2016
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Paragraph 0718-0723
(2016/10/07)
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- Pd(II)-catalyzed C(sp2)-H hydroxylation with R 2(O)P-coordinating group
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A novel R2(O)P-directed Pd(II)-catalyzed C-H hydroxylation to synthesize various substituted 2′-phosphorylbiphenyl-2-ol compounds is described. Notably, the reaction operates under mild conditions and shows good functional group tolerance, high selectivity, and yield.
- Zhang, Hong-Yu,Yi, Hong-Ming,Wang, Gang-Wei,Yang, Bin,Yang, Shang-Dong
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supporting information
p. 6186 - 6189
(2014/01/17)
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- PIPERIDINE AND MORPHOLINE RENIN INHIBITORS
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Described are compounds which are orally active and bind to renin to inhibit its activity. They are useful in the treatment or amelioration of diseases associated with renin activity. Also described are methods of use of these compounds for treating or ameliorating a renin mediated disorder in a subject.
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Page/Page column 170
(2008/06/13)
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- COMBINATIONS COMPRISING AN Hsp90 INHIBITOR AND A PHOPHODIESTERASE INHIBITOR FOR TREATING OR PREVENTING NEOPLASIA
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A method for treating or preventing neoplasia or a neoplasia-related disorder in a subject is provided, the method comprising administering to the subject an effective amount of a combination comprising an Hsp90 inhibitor and a phosphodiesterase inhibitor, and optionally a Cox-2 inhibitor.
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Page/Page column 164-165
(2008/06/13)
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- TREATMENT OR PREVENTION OF NEOPLASIA BY USE OF AN Hsp90 INHIBITOR
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A method for treating or preventing neoplasia or a neoplasia-related disorder in a subject is provided, the method comprising administering to the subject an effective amount of an Hsp90 inhibitor, or of a combination comprising an Hsp90 inhibitor and a Cox-2 inhibitor.
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Page/Page column 162-163
(2008/06/13)
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- Substituted terphenyl compounds for the treatment of inflammation
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A class of terphenyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II: STR1 wherein each of R2 and R3 is independently selected from hydrido and halo; or wherein R2 and R3 together form --OCH2 O--; wherein each of R6 through R8 is independently selected from hydrido, lower alkyl, halo, lower alkoxy, lower haloalkyl, and lower dialkylamino; or wherein R6 and R7 together form --OCH2 O; and wherein R12 is selected from lower alkylsulfonyl and aminosulfonyl; or a pharmaceutically-acceptable salt thereof.
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- Phase-Transfer-Catalyzed Gomberg-Bachmann Synthesis of Unsymmetrical Biarenes: A Survey of Catalysts and Substrates
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Two problems have hindered the Gomberg-Bachmann (GB) and Pschorr reactions of arenediazonium cations: the instability of the arenediazonium salts and side reactions.Arenediazonium tetrafluoroborate and hexafluorophosphate salts can be prepared in high yield and purity and can be stored safely.Unfortunately, these salts are insoluble in most nonpolar organic solvents.Crown ether complexation or other phase-transfer (pt) catalytic methodology can ameliorate this situation, and reactions conducted by the approaches outlined herein often afforded coupling or cyclization products in high yield and corresponding purity.The use of crown ethers, quarternary 'onium salts, lipophilic carboxylic acid salts, and even the polar cosolvent acetonitrile increase the utility of the ptGB reaction dramatically.Sixty examples of couplings are reported along with an assessment of selectivities.A number of examples are also presented of phase-transfer-type Pschorr cyclizations.In the latter case, the use of potassium superoxide, KO2, is introduced to suppress indazole formation.
- Beadle, James R.,Korzeniowsky, Stephen H.,Rosenberg, David E.,Garcia-Slanga, Blanche J.,Gokel, George W.
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p. 1594 - 1603
(2007/10/02)
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