- Synthesis of new N-pyrrolylphosphane and its application in hydroformylation of 1-octene
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A new bidentate N-pyrrolylphosphane (1) which possessing strong π-acceptor property has been synthesized and applied in homogeneous rhodium-catalyzed hydroformylation of 1-octene. The effects of ligand/metal ratio, temperature, pressure and substrate/rhod
- Zhang,Li,Zheng,Li,Chen
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- Synthesis of benzo[a]carbazoles and indolo[2,3-a]carbazoles via photoinduced carbene-mediated C-H insertion reaction
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A new synthesis of 5-hydroxy-benzo[a]carbazoles has been achieved by employing the photoinduced intramolecular C-H insertion of 2-aryl-3-(α- diazocarbonyl)indoles as the key step. This method is applicable to the synthesis of natural products 6-cyano-5-me
- Yang, Jidong,Zhang, Qingzhao,Zhang, Wei,Yu, Wei
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- Copper-Catalyzed Ullmann-Type Coupling and Decarboxylation Cascade of Arylhalides with Malonates to Access α-Aryl Esters
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We have developed a high-efficiency and practical Cu-catalyzed cross-coupling to directly construct versatile α-aryl-esters by utilizing readily available aryl bromides (or chlorides) and malonates. These gram-scale approaches occur with turnovers of up to 1560 and are smoothly conducted by the usage of a low catalyst loading, a new available ligand, and a green solvent. A variety of functional groups are tolerated, and the application occurs with α-aryl-esters to access nonsteroidal anti-inflammatory drugs (NSAIDs) on the gram scale.
- Cheng, Fei,Chen, Tao,Huang, Yin-Qiu,Li, Jia-Wei,Zhou, Chen,Xiao, Xiao,Chen, Fen-Er
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supporting information
p. 115 - 120
(2022/01/04)
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- METHOD FOR CONVERTING HYDROXYL GROUP OF ALCOHOL
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The present invention relates to: a method for converting a hydroxyl group of an alcohol; and a catalyst which makes the method possible. A method for converting a hydroxyl group of an alcohol according to the present invention is characterized by producing a compound represented by CH(R1)(R2)Nu (wherein R1, R2 and Nu are as defined below) by reacting an alcohol represented by CH(R1)(R2)OH (wherein each of R1 and R2 represents a hydrogen atom, an optionally substituted alkyl group, or the like) and a compound having an active proton, which is represented by H-Nu (wherein Nu represents a group represented by —CHX1-EWG1 or —NR3R4; X1 represents a hydrogen atom or the like; EWG1 represents an electron-withdrawing group; and each of R3 and R4 represents a hydrogen atom, an optionally substituted alkyl group, or the like), with each other in the presence of a complex of a group 7-11 metal of the periodic table and at least one solid base that is selected from the group consisting of layered double hydroxides, composite oxides and calcium hydroxide.
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Paragraph 0382-0384
(2021/02/19)
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- Highly productive α-alkylation of ketones with alcohols mediated by an Ir-oxalamidato/solid base catalyst system
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An Ir-oxalamidato complex in combination with a solid base (e.g., magnesium aluminometasilicate/Ca(OH)2) significantly improved the catalyst productivity in α-alkylation of methyl ketones with primary alcohols. Optimization through systematic variation of the oxalamidato ligand led to a practical turnover number (TON) of 10 000.40 000.
- Maeda, Hironori,Nara, Hideki,Shimizu, Hideo
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supporting information
p. 2772 - 2779
(2020/12/29)
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- Reagent Design and Ligand Evolution for the Development of a Mild Copper-Catalyzed Hydroxylation Reaction
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Parallel synthesis and mass-directed purification of a modular ligand library, high-throughput experimentation, and rational ligand evolution have led to a novel copper catalyst for the synthesis of phenols with a traceless hydroxide surrogate. The mild reaction conditions reported here enable the late-stage synthesis of numerous complex, druglike phenols.
- Fier, Patrick S.,Maloney, Kevin M.
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supporting information
p. 3033 - 3036
(2017/06/07)
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- CO-use CO2 Method for synthesizing N, N - dialkyl oxalate
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The invention provides a method for synthesizing N,N-dialkyl oxamide by using CO2. According to the method, in an organic or inorganic solvent, one-step synthetic reaction is performed on the CO2 and organic amine to synthesize the N,N-dialkyl oxamide, with N,N-dialkyl urea and water as byproducts, in the presence of a certain catalyst and under a certain reaction condition that the reaction pressure is 10-80atm and the reaction temperature is 100-200 DEG C. The invention discloses the method for synthesizing the N,N-dialkyl oxamide by using the CO2. According to the method, a valuable and toxic metal catalyst and a toxic and explosive gas in the prior art are not used, and reactants, products, and added components in a system are safe and environment-friendly; the yield is considerable; technically, an improvement room exists; a safe and environment-friendly new method is provided for preparing the N,N-dialkyl oxamide.
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Paragraph 0037; 0038; 0039; 0040; 0041
(2016/11/17)
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- Ligand-based modelling followed by synthetic exploration unveil novel glycogen phosphorylase inhibitory leads
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Glycogen phosphorylase (GP) is a valid anti-diabetic target. Accordingly, we applied a drug discovery workflow to unveil novel inhibitory GP leads via combining pharmacophore modeling, QSAR analysis and in silico screening, followed by synthetic exploration of active hits. Virtual screening identified six low micromolar inhibitory leads from the National Cancer Institute (NCI) list of compounds. The most potent hits exhibited anti-GP IC50 values of 3.2 and 4.1 μM. Synthetic exploration of hit 59 (IC50 = 4.1 μM) yielded 25 lead inhibitors with the best illustrating IC50 of 3.0 μM. Interestingly, we prepared several novel mixed oxalyl amide anti-GP leads employing new chemical reaction involving succinic acid-based adducts.
- Habash, Maha,Taha, Mutasem O.
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experimental part
p. 4746 - 4771
(2011/09/20)
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- ORGANOMETALLIC RUTHENIUM COMPLEXES AND RELATED METHODS FOR THE PREPARATION OF TETRA-SUBSTITUTED AND OTHER HINDERED OLEFINS
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The invention relates to ruthenium alkylidene complexes having an N-heterocyclic carbene ligand comprising a 5-membered heterocyclic ring having a carbenic carbon atom and at least one nitrogen atom contained within the 5-membered heterocyclic ring, wherein the nitrogen atom is directly attached to the carbenic carbon atom and is substituted by a phenyl ring, and wherein the phenyl ring has a hydrogen at either or both ortho positions and is substituted and at least one orthq or meta position. The invention also relates to an olefin metathesis reactions and particularly to the preparation of tetra-substituted cyclic olefins via a ring-closing metathesis.
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Page/Page column 19
(2010/11/27)
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- Highly efficient ruthenium catalysts for the formation of tetrasubstituted olefins via Ring-Closing Metathesis
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Equation presented A series of ruthenium-based metathesis catalysts with N-heterocyclic carbene (NHC) ligands have been prepared in which the N-aryl groups have been changed from mesityl to mono-ortho-substituted phenyl (e.g., tolyl). These new catalysts
- Stewart, Ian C.,Ung, Thay,Pletnev, Alexandre A.,Berlin, Jacob M.,Grubbs, Robert H.,Schrodi, Yann
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p. 1589 - 1592
(2008/02/03)
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- Benzannulation reactions of Fischer carbene complexes for the synthesis of indolocarbazoles
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The synthesis of indolocarbazoles was achieved via photochemical and thermal annulation reactions of chromium Fischer carbene complexes. This methodology allows for facile incorporation of hydrogen bonding functionality which complements the pharmacophore contained within bioactive indolocarbazole natural products.
- Merlic, Craig A.,You, Ying,McInnes, Daniel M.,Zechman, Andrea L.,Miller, Michael M.,Deng, Qiaolin
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p. 5199 - 5212
(2007/10/03)
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- Synthesis of N,N′-diarylalkanediamides and their antimycobacterial and antialgal activity
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A set of N,N′-diarylalkanediamides was synthesized. The compounds were tested for their antimycobacterial and antialgal activity. The antimycobacterial activity of N,N′-diarylalkanediamides depends on the lipophilicity of the respective acid. Antimycobacteri-ally active substances were found only in the series of N,N′-diarylethanediamides and N,N′-diarylbutanediamides. Other compounds (derivatives of pentane-, hexane-, octane- and nonanediamide) were inactive against various strains of mycobacteria. The compounds inhibited growth and chlorophyll production in Chlorella vulgaris. Their relatively low antial-gal activity is probably connected with their lowered aqueous solubility, and hence by a restricted passage of the inhibitor through the hydrophilic regions of thylakoid membranes.
- Kubicova, Lenka,Waisser, Karel,Kunes, Jiri,Kralova, Katarina,Odlerova, Zelmira,Slosarek, Milan,Janota, Jiri,Svoboda, Zbynek
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p. 714 - 726
(2007/10/03)
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- On the Cycloaddition Approach to Indolocarbazoles
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2,2'-Biindolyl 9 reacts with electron-deficient dienophiles at 100-110 deg C to give low to moderate yields of Michael addition and formal cycloaddition products, with the former predominant; the products derived from 9 and 2-(phenylsulphinyl)maleimides 14 and 15 undergo in situ elimination of benzenesulphenic acid, leading to 2,2'-biindolyl-substituted maleimides which can be efficiently photocyclised into indolocarbazoles.
- Barry, John F.,Wallace, Timothy W.,Walshe, Nigel D. A.
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p. 12797 - 12806
(2007/10/02)
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