- Alkyl-GeMe3: Neutral Metalloid Radical Precursors upon Visible-Light Photocatalysis
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Single-electron transfer (SET) oxidation of ionic hypervalent complexes, in particular alkyltrifluoroborates (Alkyl-BF3?) and alkylbis(catecholato)silicates (Alkyl-Si(cat)2?), have contributed substantially to alkyl radical generation compared to alkali or alkaline earth organometallics because of their excellent activity–stability balance. Herein, another proposal is reported by using neutral metalloid compounds, Alkyl-GeMe3, as radical precursors. Alkyl-GeMe3 shows comparable activity to that of Alkyl-BF3? and Alkyl-Si(cat)2? in radical addition reactions. Moreover, Alkyl-GeMe3 is the first successful group 14 tetraalkyl nucleophile in nickel-catalyzed cross-coupling. Meanwhile, the neutral nature of these organogermanes offset the limitation of ionic precursors in purification and derivatization. A preliminary mechanism study suggests that an alkyl radical is generated from a tetraalkylgermane radical cation with the assistance of a nucleophile, which may also result in the development of more non-ionic alkyl radical precursors with a metalloid center.
- Wei, Li-Pu,Xiao, Bin,Xu, Qing-Hao
-
supporting information
(2022/02/17)
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- Dealkenylative Ni-Catalyzed Cross-Coupling Enabled by Tetrazine and Photoexcitation
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A new and general method to functionalize the C(sp3)-C(sp2) bond of alkyl and alkene linkages has been developed, leading to the dealkenylative generation of carbon-centered radicals that can be intercepted to undergo Ni-catalyzed C(sp3)-C(sp2) cross-coupling. This one-pot protocol leverages the easily procured alkene feedstocks for organic synthesis with excellent functional group compatibility without the need for a photoredox catalyst.
- Cao, Yuhui,Che, Jinteng,Chen, Han,Chen, Si-Cong,Fang, Xianhe,Guo, Yinliang,Guo, Zhixian,Kong, Lingran,Li, Chen,Lu, Jia-Tian,Luo, Tuoping,Zhang, Nan,Zhu, Qi
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p. 14046 - 14052
(2021/09/13)
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- Micelle enabled C(sp2)-C(sp3) cross-electrophile coupling in waterviasynergistic nickel and copper catalysis
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A robust and sustainable C(sp2)-C(sp3) cross-electrophile coupling was developedvianickel/copper synergistic catalysis under micellar conditions. This protocol provided a general method to access alkylated arenes with good to excellent yields on a very large scale.
- Ye, Ning,Wu, Bin,Zhao, Kangming,Ge, Xiaobin,Zheng, Yu,Shen, Xiaodong,Shi, Lei,Cortes-Clerget, Margery,Regnier, Morgan Louis,Parmentier, Michael,Gallou, Fabrice
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supporting information
p. 7629 - 7632
(2021/08/09)
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- COMPOSITION FOR FORMING RESIST UNDERLAYER FILM AND METHOD FOR FORMING PATTERN
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The invention provides a composition for forming a resist underlayer film, comprising a compound represented by the formula (I): [LxTe(OR 1 )y] (1) (in formula (1), L is a ligand other than OR 1 R 1 is any of hydrogen atom, substituted or unsubstituted linear alkyl having 1 to 20 carbon atom or substituted or unsubstituted branched or cyclic alkyl having 3 to 20 carbon atoms, substituted or unsubstituted aryl having 6 to 20 carbon atoms, and substituted or unsubstituted alkenyl having 2 to 20 carbon atoms x is an integer of 0 to 6 y is an integer of 0 to 6 the sum of x and y is 1 to 6 a plurality of L may be the same or different when x is 2 or more and a plurality of R 1 may be the same or different when y is 2 or more).
- -
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Paragraph 0131-0133
(2020/04/29)
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- COMPOSITION FOR RESIST UNDERLAYER FILM FORMATION, UNDERLAYER FILM FOR LITHOGRAPHY, AND PATTERN FORMATION METHOD
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The present invention provides a composition for resist underlayer film formation comprising a tellurium-containing compound or a tellurium-containing resin.
- -
-
Paragraph 0561; 0563-0565
(2020/08/22)
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- COMPOUNDS AND METHOD OF USE
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This present disclosure relates to compounds with ferroptosis inducing activity, a method of treating a subject with cancer with the compounds, and combination treatments with a second therapeutic agent.
- -
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Paragraph 1198
(2019/09/06)
-
- Method for synthesizing aromatic aldehyde through iron catalyzed oxidation allyl aromatic compound
-
The invention discloses a method for synthesizing aromatic aldehyde through an iron catalyzed oxidation allyl aromatic compound. According to the specific method, under the promotion effect of hydrogen silane, with air or oxygen as the oxidant, the aromatic aldehyde compound is synthesized through the iron catalyzed oxidation allyl aromatic compound, the reaction temperature is 20-150 DEG C, and the time is 0.25-60 h. The method has the advantages that a catalyst source is wide, the price is low and the environment is protected; an oxidant source is wide, the price is low and no waste is generated; the reaction conditions are mild, selectivity is high and the yield is high; a substrate source is wide and stable; a substrate functional group is high in compatibility and a substrate is widein application range; complicated small molecules are compatible and can be well converted into aldehyde. The target product separation yield can reach up to 96% under the optimized reaction conditions.
- -
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Paragraph 0093-0095; 0150
(2019/06/27)
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- Ni-catalyzed Reductive Deaminative Arylation at sp3 Carbon Centers
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A Ni-catalyzed reductive deaminative arylation at unactivated sp3 carbon centers is described. This operationally simple and user-friendly protocol exhibits excellent chemoselectivity profile and broad substrate scope, thus complementing existing metal-catalyzed cross-coupling reactions to forge sp3 C-C linkages. These virtues have been assessed in the context of late-stage functionalization, hence providing a strategic advantage to reliably generate structure diversity with amine-containing drugs.
- Martin-Montero, Raul,Yatham, Veera Reddy,Yin, Hongfei,Davies, Jacob,Martin, Ruben
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p. 2947 - 2951
(2019/04/30)
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- Palladium-Catalyzed para-Selective Alkylation of Electron-Deficient Arenes
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Intermolecular alkylations of electron-deficient arenes proceed with good para selectivity. Palladium catalysts were used to generate nucleophilic alkyl radicals from alkyl halides, which then directly add onto the arenes. The arene scope and the site of
- Jiao, Zhiwei,Lim, Li Hui,Hirao, Hajime,Zhou, Jianrong Steve
-
supporting information
p. 6294 - 6298
(2018/05/30)
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- FARNESOID X RECEPTOR AGONISTS AND USES THEREOF
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Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.
- -
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Paragraph 00401
(2017/04/11)
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- RESIST COMPOSITION AND METHOD FOR FORMING PATTERN
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The present invention relates to a resist composition comprising a compound having a specific structure. The compound has high heat resistance derived from its skeleton having high aromaticity while has low molecular weight, thus it can be used for baking at a high temperature. Due to the specific structure, the resist composition of the present invention is excellent in resistance to heat and high in solubility to safe solvents, thereby imparting to the resultant resist pattern high sensitivity and excellent resistance to etching. Therefore, the resist composition of the present invention is useful as acid amplified non-polymeric resist material.
- -
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Paragraph 0219
(2016/12/01)
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- RESIST COMPOSITION, METHOD FOR FORMING RESIST PATTERN, POLYPHENOLIC COMPOUND FOR USE IN THE COMPOSITION, AND ALCOHOLIC COMPOUND THAT CAN BE DERIVED THEREFROM
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A resist composition containing a compound represented by the general formula (1) or (2), a method for forming a resist pattern using the composition, a polyphenolic compound for use in the composition, and an alcoholic compound that can be derived therefrom are described.
- -
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Paragraph 0519-0522
(2016/06/13)
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- Structure-activity relationship study of E6 as a novel necroptosis inducer
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Necroptosis inducers represent a promising potential treatment for drug-resistant cancer. We herein describe the structure modification of E6, which was identified recently as a potent and selective necroptosis inducer. The studies described herein demonstrate for the first time that functionalized biphenyl derivatives possess necroptosis inducer activity. Furthermore, these studies have led to the identification of two promising compounds (5h and 5j) that can be used for further optimization studies as well as mechanism of action investigations.
- Mou, Jianfeng,Park, Ann,Cai, Yu,Yuan, Junying,Yuan, Chengye
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supporting information
p. 3057 - 3061
(2015/06/22)
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- Alkylations of Arylboronic Acids including Difluoroethylation/Trifluoroethylation via Nickel-Catalyzed Suzuki Cross-Coupling Reaction
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An efficient alkylation method of functionalized alkyl halides under mild nickel-catalyzed C(sp3)-(sp2) Suzuki cross-coupling conditions is described. The features of this approach are excellent functional group compatibility, low cost nickel catalyst, and the use of a mild base. This is also the first successful example of the nickel-catalyzed direct 2,2-difluoroethylation or 2,2,2-trifluoroethylation of aryl-/heteroarylboronic acids.
- Zhang, Xiaofei,Yang, Chunhao
-
supporting information
p. 2721 - 2727
(2015/09/01)
-
- Identification of bidentate salicylic acid inhibitors of PTP1B
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PTP1B is a master regulator in the insulin and leptin metabolic pathways. Hyper-activated PTP1B results in insulin resistance and is viewed as a key factor in the onset of type II diabetes and obesity. Moreover, inhibition of PTP1B expression in cancer cells dramatically inhibits cell growth in vitro and in vivo. Herein, we report the computationally guided optimization of a salicylic acid-based PTP1B inhibitor 6, identifying new and more potent bidentate PTP1B inhibitors, such as 20h, which exhibited a > 4-fold improvement in activity. In CHO-IR cells, 20f, 20h, and 20j suppressed PTP1B activity and restored insulin receptor phosphorylation levels. Notably, 20f, which displayed a 5-fold selectivity for PTP1B over the closely related PTPσ protein, showed no inhibition of PTP-LAR, PRL2 A/S, MKPX, or papain. Finally, 20i and 20j displayed nanomolar inhibition of PTPσ, representing interesting lead compounds for further investigation.
- Haftchenary, Sina,Jouk, Andriana O.,Aubry, Isabelle,Lewis, Andrew M.,Landry, Melissa,Ball, Daniel P.,Shouksmith, Andrew E.,Collins, Catherine V.,Tremblay, Michel L.,Gunning, Patrick T.
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supporting information
p. 982 - 986
(2015/09/22)
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- BICYCLOHEXANE DERIVATIVE AND PRODUCTION METHOD FOR SAME
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A bicyclohexane derivative compound useful in the field of photoresist, the field of intermediate of drugs and pesticides, and the like, and a manufacturing method of the same are provided. A bicyclohexane derivative compound represented by the following general formula (II) is provided. (In formula (II), Y independently represents an alkyl group of 1 to 10 carbons, a halogen atom, an acyloxy group, an alkoxycarbonyl group or a hydroxyl group, X1 represents a halogen atom, m represents an integer of 0 to 11, and m' represents an integer of 0 to 10.)
- -
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Page/Page column 22
(2012/12/13)
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- Discovery of naturally occurring aurones that are potent allosteric inhibitors of hepatitis C virus RNA-dependent RNA polymerase
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We have identified naturally occurring 2-benzylidenebenzofuran-3-ones (aurones) as new templates for non-nucleoside hepatitis C virus (HCV) RNA-dependent RNA polymerase (RdRp) inhibitors. The aurone target site, identified by site-directed mutagenesis, is located in thumb pocket I of HCV RdRp. The RdRp inhibitory activity of 42 aurones was rationally explored in an enzyme assay. Molecular docking studies were used to determine how aurones bind to HCV RdRp and to predict their range of inhibitory activity. Seven aurone derivatives were found to have potent inhibitory effects on HCV RdRp, with IC50 below 5 μM and excellent selectivity index (inhibition activity versus cellular cytotoxicity). The most active aurone analogue was (Z)-2-((1-butyl-1H-indol-3-yl)methylene)-4,6-dihydroxybenzofuran-3(2H)-one (compound 51), with an IC50 of 2.2 μM. Their potent RdRp inhibitory activity and their low toxicity make these molecules attractive candidates as direct-acting anti-HCV agents.
- Haudecoeur, Romain,Ahmed-Belkacem, Abdelhakim,Yi, Wei,Fortuné, Antoine,Brillet, Rozenn,Belle, Catherine,Nicolle, Edwige,Pallier, Coralie,Pawlotsky, Jean-Michel,Boumendjel, Ahcène
-
body text
p. 5395 - 5402
(2011/10/02)
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- PDE-10 INHIBITORS
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Vicinal substituted cyclopropyl compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function, for example neurological, neurodegenerative and psychiatric disorders including, but not limited to, those comprising cognitive deficits or schizophrenic symptoms.
- -
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Page/Page column 32-33
(2010/04/03)
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- RADIATION-SENSITIVE COMPOSITION
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A radiation-sensitive composition containing a resist compound having a high sensitivity, a high resolution, a high etching resistance, and a low outgas which forms a resist pattern with a good shape is described. Further described is a method of forming a resist pattern using the radiation-sensitive composition. Still further described are a novel composition for forming a photoresist under coat film which is excellent in optical properties and etching resistance and contains substantially no sublimable substance and an under coat film formed by the composition. Still further described are a radiation-sensitive composition containing a solvent and a cyclic compound having a specific structure, for example, a cyclic compound (A) having a molecular weight of 700 to 5000 which is synthesized by the condensation reaction of a compound having 2 to 59 carbon atoms and 1 to 4 formyl groups (aldehyde compound (A1)) with a compound having 6 to 15 carbon atoms and 1 to 3 phenolic hydroxyl groups (phenol compound (A2)), and a cyclic compound for use in the radiation-sensitive composition.
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Page/Page column 103
(2009/08/14)
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- PHARMACEUTICAL PREPARATIONS COMPRISING INSULIN, ZINC IONS AND A ZINC-BINDING LIGAND
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Novel preparations comprising branched ligands for the HisB10 Zn2+ sites of the R-state insulin hexamer. The preparations have a prolonged action designed for flexible injection regimes.
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Page/Page column 182
(2008/06/13)
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- PHAMACEUTICAL PREPARATIONS COMPRISING INSULIN
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Novel preparations comprising ligands for the HisB10 Zn2+ sites of the R-state insulin hexamer wherein the ligand is extended by protamine that are capable of prolonging the ac-tion of insulin preparations.
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Page/Page column 177
(2010/02/15)
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- Stabilised insulin compositions
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The present invention provides pharmaceutical compositions comprising insulin and novel ligands for the HisB10 Zn2+ sites of the R-state insulin hexamer. The resulting preparations have improved physical and chemical stability.
- -
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Page/Page column 86
(2008/06/13)
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- AZOLE COMPOUND AND MEDICINAL USE THEREOF
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The present invention relates to an azole compound represented by the formula [I] wherein W is S or O; R is -COOR7, -X1-A1-COOR7 (R7 is H, alkyl) or tetrazolyl; R1, R2, R3 and R4 are H and the like; A is -(CH2)m-X- (X is -N(R8)-, -C(R9)(R10)-, -CO- or -CO-N(R8)-); B is aryl or aromatic heterocyclic group; R5 is H and the like; R6 is -(Y)s1-(A2)s-Z (Y is -O-, -S(O)t-, -N(R13)-, -N(R14)-CO-, -N(R14)-SO2-, -SO2-N(R14)- and the like, A2 is alkylene, and Z is cycloalkyl, aryl, aromatic heterocyclic group, indanyl, piperazinyl, a prodrug thereof or a pharmaceutically acceptable salt thereof. The compound [I] of the present invention has a protein tyrosine phosphatase 1B inhibitory activity, and is useful as a therapeutic agent for diabetes, a therapeutic drug for diabetic complications or a therapeutic drug for hyperlipidemia.
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-
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- FUROISOQUINOLINE DERIVATIVES, PROCESS FOR PRODUCING THE SAME AND USE THEREOF
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A compound having a partial structure represented by Formula: or a salt thereof has an excellent phosphodiesterase (PDE) IV-inhibiting effect, and is useful as a prophylactic or therapeutic agent against inflammatory diseases, for example, bronchial asthma, chronic obstructive pulmonary disease (COPD), rheumatoid arthritis, autoimmune disease, diabetes and the like.
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-
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- One-pot three-step solution phase syntheses of thiohydantoins using microwave heating
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An efficient one-pot three-step solution phase protocol suitable for library syntheses of thiohydantoins was developed. The reactions included are in the following order, Negishi or Suzuki C-C coupling reactions, reductive amination and finally a cyclisation reaction. Protocols using a solid supported reagent and protocols suitable for combinatorial chemistry were developed, all including microwave heating.
- ?hberg,Westman
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p. 1893 - 1896
(2007/10/03)
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- Methods and compounds for inhibiting β-amyloid peptide release and/or its synthesis
-
Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
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-
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- Compounds for inhibiting β-amyloid peptide release and/or its synthesis
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Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis.
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-
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- Compounds for inhibiting β-amyloid peptide release and/or its synthesis
-
Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis.
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-
- Orthoamides. LIII. A New Synthesis for Aromatic Aldehydes of Wide Scope
-
Diformamide (1) reacts with activated aromatic compounds like toluene, anisole, m-xylene, 1,2-dimethoxybenzene in the presence of AlCl3 to give N-(diarylmethyl)-formamides 2a-d, the corresponding aromatic aldehydes 3-6 are formed as by-products in low yields. From N,N-dimethylaniline and 1/AlCl3 the triphenylmethane derivative 7 can be obtained. The reaction of anisole with N-methyl-diformamide (9) affords the formamide 10. The mixture of formamide, P4O10 and AlCl3 reveals to be a reagent which is capable to formylate toluene and anisole, resp. Triformamide (14)/AlCl3 is an effective formylating system which allows the preparation of aromatic aldehydes (e.g. 3,4,17-32) from the corresponding aromatic hydrocarbons. Aluminiumchloride can be replaced by borontrichloride. The yields of the formylation reactions depend strongly from the reaction conditions (molar ratio: aromatic hydrocarbon/ AlCl3/14; solvent, reaction temperature). The scope of the reaction covers nearly complete those of the Gattermann-Koch-, Gattermann- and Vilsmeier-Haack-reaction.
- Kantlehner, Willi,Vettel, Markus,Gissel, Alexander,Haug, Erwin,Ziegler, Georg,Ciesielski, Michael,Scherr, Oliver,Haas, Richard
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p. 297 - 310
(2007/10/03)
-
- Manganese-catalyzed substitution of activated aryl halides (X = Cl, Br and F) and aryl ethers by organomagnesium reagents
-
In the presence of manganese chloride (10%), Grignard reagents readily react in THF with aryl bromides, chlorides and even fluorides, as well as aryl methyl ethers bearing in the ortho- or para-position an electron withdrawing activating group (CN, CH=NR, oxazoline). Aryl and N- or S- alkylmagnesium halides have been used successfully. The reaction is performed under mild conditions (0 °C to room temperature, 30 minutes to 24 hours) and leads to cross-coupling products in good yields.
- Cahiez, Gerard,Lepifre, Franck,Ramiandrasoa, Parfait
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p. 2138 - 2144
(2007/10/03)
-
- Synthesis of Certain Mesogenic Azomethines Derived from 4-Cycloalkylanilines and from 4-Cycloalkylbenzaldehydes
-
General procedures are described for the synthesis of members of five pairs of related homologous series of mesogenic azomethines differing in the mode of linkage of the CH=N group and containing a cycloalkyl group in a terminal position.
- Byron, D. J.,Matharu, A. S.,Rees, M.,Wilson, R. C.
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p. 229 - 238
(2007/10/02)
-
- Synthesis and Antimalarial Properties of 1-Imino Derivatives of 7-Chloro-3-substituted-3,4-dihydro-1,9(2H,10H)-acridinediones and Related Structures
-
To improve upon the activity and properties of the 3-aryl-7-chloro-3,4-dihydro-1,9(2H,10H)-acridinediones, a variety of 1-imino derivatives (3) were prepared and shown to be highly active antimalarial agents in both rodents and primates.Among structural modifications prepared, including N10-alkyl and C2-substituted analogs, removal of the C9 oxygen, and introduction of an imino side chain at C9, the imines of the N10-H acridinediones were the most active compounds obtained.The imino derivative of7-chloro-3-(2,4-dichlorophenyl)-3,4-dihydro-1,9(2H,10H)-acridinedione (9aa) proved to be highly active in advanced studies in primates.
- Kesten, Stephen J.,Degnan, Margaret J.,Hung, Jocelyn,McNamara, Dennis J.,Ortwine, Daniel F.,et al.
-
p. 3429 - 3447
(2007/10/02)
-
- Properties of the Liquid Crystals Formed by Ceratin Azomethines Derived from 4-Cycloalkylanilines and from 4-Cycloalkylbenzaldehydes
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The liquid crystal behaviour of four homologous series of azomethines related to the nO.m series but containing a cycloalkyl group, is reported and discussed.Many of these compounds show extensive smectic polymorphism, one member of the nO.c6 series giving rise to five smectic polymorphic modofications for which phase type assignments have been made by thermal optical microscopy.Keywords: smectic polymorphism, azomethines, cycloalkyl derivatives
- Brown, J. W.,Byron, D. J.,Southcott, M.,Wilson, R. C.,Guillon, D.,et al.
-
-
- Formylation and Acylation Reactions Catalysed by Trifluoromethanesulphonic Acid
-
Regioselective formylation of toluene, m- and p-xylene, and mesitylene has been achieved by carbonylation in trifluoromethanesulphonic acid at CO pressures of 90-125 atm.In the case of cumene, the formylation reaction is in competition with disproportionation to form di- and tri-isopropylbenzenes, leading to a complex product mixture.Slow addition of cyclohexene or cyclopentene to a mixture of benzene and CF3SO3H under a high CO pressure affords 4-cyclohexylbenzaldehyde and 4-cyclopentylbenzaldehyde in 34percent and 33percent yieds, respectively, while 2-methylbut-1-ene gives 2,2,3-trimethylindanone (39percent) under similar conditions.When cyclohexene is mixed with the acid under carbon monoxide (120 atm) before addition of benzene the major products are cyclohexyl phenyl ketone and cyclohexenyl cyclohexyl ketones.
- Booth, Brian L.,El-Fekky, Teymour A.,Noori, Ghazi F. M.
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p. 181 - 186
(2007/10/02)
-
- Synthesis of new esters of prednisolone and triamcinolone acetonide and investigation of their antiinflammatory activity
-
17 Acids with diphenylyl and cyclohexylphenyl groups were esterified with the hydroxyl group at position 21 of prednisolone and triamcinolone acetonide. Some of these esters showed marked activity against carrageenin edema and Selye spots in the rat, especially on local application.
- Carenini,Carissimi,D'Ambrosio,Ravenna
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p. 167 - 184
(2007/10/10)
-