- Room-Temperature Palladium(II)-Catalyzed Direct 2-Arylation of Indoles with Tetraarylstannanes
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A palladium(II)-catalyzed direct 2-arylation of indoles by tetraarylstannanes with oxygen (balloon) as the oxidant at room temperature has been developed. Various tetraarylstannanes can be employed as aryl sources for 2-arylation of indoles in up to 89% yield, providing a practical and efficient catalytic protocol for accessing 2-arylindoles.
- Liu, Yuxia,Wang, Chao,Huang, Linjuan,Xue, Dong
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supporting information
p. 1613 - 1618
(2020/09/15)
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- A method for preparing substituted biphenyl
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The invention discloses a preparation method of substituted biphenyl. The preparation method includes the steps that under the anhydrous condition, a compound 2 and a compound 3 are subjected to a coupled reaction in solvent in the presence of Ni salt and ZnX3X4, and then substituted biphenyl is obtained, wherein Ni salt is one or more of NiX5X6(PPh3)2, NiX7X8(dppp), NiX9X10(dppf), NiX11X12(dppe) and acetylacetone nickel, the temperature of the coupled reaction is 0-30 DEG C, and ZnX3X4 is mixed with the compound 3 before the compound 2 is mixed with the compound 3. According to the method, reaction conditions are mild, the process is simple, operation is safe, requirements for equipment are low, aftertreatment is simple, pollution to the environment is small, industrial production is easy, the usage quantity of zinc halides is small, the cost is low, the yield is high, and the product purity is high.
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Paragraph 0114; 0115; 0116; 0124; 0125; 0126
(2018/08/03)
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- Nickel-Catalyzed Cross-Coupling of Functionalized Organo manganese Reagents with Aryl and Heteroaryl Halides Promoted by 4-Fluorostyrene
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A catalytic system consisting of Ni(acac) 2 (5 mol%) and 4-fluorostyrene (20 mol%) allows a convenient cross-coupling of functionalized organomanganese reagents with a variety of aryl and heteroaryl halides leading to polyfunctionalized diaryl- and arylheteroarylmethane derivatives.
- Benischke, Andreas D.,Desaintjean, Alexandre,Juli, Thomas,Cahiez, Gérard,Knochel, Paul
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supporting information
p. 5396 - 5412
(2017/12/14)
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- Nickel-Catalyzed Asymmetric Kumada Cross-Coupling of Symmetric Cyclic Sulfates
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Nickel-catalyzed enantioselective cross-couplings between symmetric cyclic sulfates and aromatic Grignard reagents are described. These reactions are effective with a broad range of substituted cyclic sulfates and deliver products with asymmetric tertiary carbon centers. Mechanistic experiments point to a stereoinvertive SN2-like oxidative addition of a nickel complex to the electrophilic substrate.
- Eno, Meredith S.,Lu, Alexander,Morken, James P.
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supporting information
p. 7824 - 7827
(2016/07/11)
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- Palladium-catalyzed aerobic oxidative double allylic C-H oxygenation of alkenes: A novel and straightforward route to α,β-unsaturated esters
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A mild tandem oxidative functionalization of allyl aromatic hydrocarbons was accomplished using the catalytic system of Pd(OAc)2/DMA under 1 atm O2. The green twofold C-O bond formation involving double allylic C-H oxygenation unlocks opportunities for markedly different synthetic strategies. Moreover, the reaction affords aryl α,β-unsaturated esters directly from readily available terminal olefins in moderate to good yields with excellent chemo- and stereoselectivities.
- Yang, Wanfei,Chen, Huoji,Li, Jianxiao,Li, Chunsheng,Wu, Wanqing,Jiang, Huanfeng
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supporting information
p. 9575 - 9578
(2015/06/08)
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- Bismuth-catalyzed synthesis of polycyclic aromatic hydrocarbons (PAHs) with a phenanthrene backbone via cyclization and aromatization of 2-(2-arylphenyl)vinyl ethers
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The reaction of 2-(2-arylphenyl)vinyl ethers in the presence of a catalytic amount of bismuth(III) triflate gave substituted phenanthrenes in excellent yields under mild reaction conditions. The reaction was also applied to the construction of other polycyclic aromatic hydrocarbons (PAHs), such as chrysene, helicene, and pyrene having a phenanthrene backbone, via regioselective cyclization. This method has the advantages of easy availability of the cyclization precursors, operational simplicity, and high reaction efficiency.
- Murai, Masahito,Hosokawa, Naoki,Roy, David,Takai, Kazuhiko
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supporting information
p. 4134 - 4137
(2014/09/30)
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- PROCESS FOR PRODUCING OPTICALLY ACTIVE ALCOHOL
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Disclosed is a method for producing an optically active alcohol including reacting a titanium compound, an aromatic magnesium compound and a carbonyl compound in the presence of an optically active biphenol compound having a predetermined structure and an ether compound having a predetermined structure.
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Page/Page column 20
(2012/02/14)
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- Use of73Ge NMR Spectroscopy and X-ray Crystallography for the Study of electronic interactions in substituted tetrakis(phenyl)-, -(phenoxy)-, and -(thiophenoxy)germanes
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NMR chemical shifts of 1H, 13C, and 73Ge, molecular modeling, and single-crystal X-ray diffraction results are reported for a series of substituted tris- and tetrakis(phenyl)germanes of the type (XC6H4)3GeY and (XC6H 4)4Ge, where X = o-, m-, and p-OCH3, o-, m-, and p-OC2H5, m- and p-CF3, H, p-C(CH 3)3, p-Cl; and Y = Cl and H. Chemical shifts and X-ray data are also reported for o-CH3 and o-OCH3 tetrakis(phenoxy)- ((XC6H4O)4Ge) and thiophenoxygermanes ((XC6H4S)4Ge). For tetrakis derivatives, 73Ge resonances are observed for all but the o-methoxyphenoxy compound, for which the inability to detect a resonance is attributed to rapid quadrupolar relaxation caused by intramolecular interactions of the methoxy oxygen with the central atom. The observation of a relatively broad, slightly upfield 73Ge resonance in the analogous phenyl and thiophenoxy derivatives suggests, as do the results of molecular modeling, that in these compounds there is some hypercoordination. The solid-state structures show bond angles at the aromatic carbon bearing the alkoxy group that suggest an interaction of the alkoxy oxygen with germanium. Oxygen-germanium bond distances are about 17% shorter than the sum of the van der Waals radii.
- Yoder, Claude H.,Agee, Tamara M.,Griffith, Allison K.,Schaeffer Jr., Charles D.,Carroll, Mary J.,Detoma, Alaina S.,Fleisher, Adam J.,Gettel, Cameron J.,Rheingold, Arnold L.
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experimental part
p. 582 - 590
(2010/04/25)
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- Haloperidol analogs
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Haloperidol analogs that conforms to the structural formulae: wherein: R is H, or —(CH2)n—OH, n is an integer from 0 to 2, and A is a heterocyclic bridging group, consisting essentially of carbon and at least one nitrogen atom, which effectively maintains the distance between the moieties connected thereby such that the compound (1) is incapable of metabolizing to BCPP+ like species, (2) has an affinity for the D2 receptor subtype of 151 is H, or —(CH2)n—OH, n is an integer from 0 to 2, B is an aza- or diaza-bicyclo group, which effectively maintains the distance between the moieties connected thereby such that the compound is incapable of metabolizing to BCPP+ like species; and Z is —CH— or N; and pharmaceutically acceptable salts, esters, derivatives, metal complexes, conjugates and prodrugs thereof.
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Page/Page column 5
(2008/06/13)
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- Arylzinc species by microwave assisted Grignard formation-transmetallation sequence: Application in the Negishi coupling
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Arylmagnesium species can be efficiently generated from magnesium turnings and aryl chlorides or aryl bromides under dielectric heating conditions. Subsequent microwave assisted transmetallation using ZnCl2-TMEDA afforded the corresponding arylzinc reagents. A sequential microwave assisted arylmagnesium formation-transmetallation-Negishi coupling protocol suitable for automated multiple parallel synthesis has been developed.
- Mutule, Ilga,Suna, Edgars
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p. 11168 - 11176
(2007/10/03)
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- Process for the preparation of 1,3-Dihydro-6-methylfuro(3,4-c)pyridin-7-ol Derivatives
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The present invention relates to a process for the preparation of 1,3-dihydro-6-methylfuro[3,4-c]pyridin-7-ol derivatives and salts thereof.
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- Synthesis of novel 1-(substituted phenyl)-2-phospholene 1-oxide derivatives
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Several novel 1-(substituted phenyl)-2-phospholene 1-oxide derivatives, which are analogs of sugars having a phosphorus atom in place of the ring oxygen of normal sugars, were synthesized from the corresponding 2-phospholenes as the starting materials. Structures of all the synthesized compounds were unequivocally confirmed by IR, 1H, 13C, and 31P NMR spectral, elemental, and X-ray crystallographic analyses.
- Reddy, Valluru Krishna,Rao, Lakonda Nagaprasada,Oshikawa, Tatsuo,Takahashi, Masaki,Yamashita, Mitsuji
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p. 1801 - 1806
(2007/10/03)
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- Therapeutic agents
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Compounds of formula I STR1 and pharmaceutically acceptable salts thereof in which m is an integer from 1 to 3; n is an integer from 2 to 6; R1 is phenyl optionally substituted by one or more substituents selected from halo, hydroxy, alkoxy, alkanoyl, alkyl, halogenated alkyl, alkylthio, alkylsulphinyl, alkylsulphonyl, cyano, nitro, optionally substituted amino, optionally substituted sulphamoyl, optionally substituted carbamoyl or phenyl, or R1 is naphthyl; R2 is H, alkyl or phenyl; R3 is H, alkyl, alkenyl or alkoxyalkyl; R4 is H or hydroxy; and R5 is H or together with R4 represents a bond; have utility in the treatment of obesity and affective disorders such as depression and anxiety.
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- Triazole derivatives
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The present invention relates to a novel glycerol derivative and a process for preparing the same, and a process for preparing a triazole derivative. According to the present invention, an optical active 2-arylglycerol derivative which is a novel and useful as a synthetic intermediate of medicament can be provided and furthermore, (R)-2-(2,4-difluorophenyl)-3-(1H-1,2,4-triazole-1-yl)-propane-1,2-diol which is useful as an antifungal agent can be prepared.
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- AROMATASE INHIBITING 4(5)-IMIDAZOLES
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Imidazole derivatives of the formula: where in R1, R2, R1 and R2 which can be the same or different, are H, CH3, C2 H5, OCH3, OH, CH2 OH, NH2 or halogen; R' if H or where R3 is H, CH3, or halogen; R4 is H and R5 is H or OH and R6 is H or OH or one of R5 and R6 is H and the other, together with R4, forms a bond and X and Y, which can be the same or different, are a bond, a straight C1-2 -alkyl or the corresponding alkenyl, and pharmaceutically acceptable salts thereof exhibit valuable pharmacological properties, especially aromatase inhibiting effects and are useful in the treatment of estrogen dependent diseases, e.g. breast cancer. Anti-mycotic and antifungal properties have also been found.
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- Synthesis and Liquid Crystal Behaviour of Further 4,4"-Disubstituted 2'-Fluoro-1,1':4',1"-Terphenyls
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Further to earlier work on the liquid crystal properties of fluoro-1,1':4',1"-terphenyls we have now extended this series to include terminally fluoro- and cyano-substituted 2'-fluoro-1,1':4',1"-terphenyls, chiral 2'-fluoro-1,1':4',1"-terphenyls, and esters derived from 2'-fluoro-1,1':4',1"-terphenyls and incorporating the alkylcyclobutyl group.The preparations and transition temperatures for these series of compounds are presented and their transition temperatures and mesophase types are discussed.An interesting result from this work was the appearence of an S*C phase for one chiral homologue and of SC phases for the esters incorporating the alkylcyclobutyl group.The SC formation is attributed to the presence of the fluoro-substituent.Keywords: terphenyls, fluoroterphenyls, smectic C phases, cyclobutyl esters.
- Chan, L. K. M.,Gray, G. W.,Lacey, D.,Toyne, K. J.
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p. 209 - 240
(2007/10/02)
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- Thermochemical Bond Dissociation Energies of Carbon-Magnesium Bonds
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The heats of formation of 29 alkylmagnesium bromides, isobutyl bromide, and neopentyl bromide have been determined, and bond dissociation energies have been derived for the Grignard reagents.For saturated alkyl derivatives the C-Mg bond strength decreases with an increasing number of β-hydrogens in the series methyl, neopentyl, isobutyl, butyl, ethyl, 1-ethylpropyl, 1-methylpropyl, isopropyl, and t-butyl.Bonding in alkyl bromides and alkylmagnesium bromides is discussed.
- Holm, Torkil
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p. 464 - 467
(2007/10/02)
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- N-Acyl-3-azetidinone
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Disclosed herein are novel N-acyl-3-aryl-3-azetidinols useful as intermediates. A method is provided for their direct preparation from acyclic starting materials. These N-acyl-3-aryl-azetidinols provide a convenient route to the 3-azetidinol series.
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