- Guanidinatoaluminum complexes: Synthesis, crystal structures and reactivities
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Treatment of diethylaminolithium with carbodiimide (CyNCNCy or CyNCNC6H5) and dimethylaluminium chloride (AlMe2Cl) in a molar ratio of 1:1:1 afforded two kinds of guanidinatoaluminum complexes, [{(Et2N)C(NR1)(NR2)}AlMe2] (R1, R2 = Cy (1); R1 = Cy, R2 = C6H5 (2)) and [{(Et2N)C(NCy)(NC6H5)}2AlMe] (3). The reactivities of the mononuclear guanidinatoaluminum complexes (1 and 2) with O2 or carbodiimide were studied. The complexes of [{(Et2N)C(NCy)2}AlMe(μ-OMe)]2 (4) and [{N(C6H5)C(NCy)N(C6H5)C(NEt2)N(Cy)}AlMe2] (5) were produced by introducing dry oxygen or carbodiimide (CyNCNC6H5) slowly into the solution of the mononuclear guanidinatoaluminum complex (1 or 2). Meanwhile, the addition of O2 or carbodiimide (ArNCNC6H5, Ar = 2,6-Me2C6H3) to the reaction solution of diethylaminolithium with ArNCNC6H5 and AlMe2Cl in a molar ratio of 1:1:1 yielded [(Et2N)C(NC6H5)(NAr)AlMe(μ-OMe)]2 (6) and [{N(C6H5)C(NAr)N(C6H5)C(NEt2)N(Ar)}AlMe2] (7). In addition, a one-pot reaction of diethylaminolithium with CyNCNCy and AlMe2Cl in a molar ratio of 1:1:1 in the presence of H2O produced a tetranuclear guanidinatoaluminum complex, (8), which was also prepared by treatment of complex 1 with equivalent AlMe3 and H2O in 35% yield. All complexes 1-8 were characterized by 1H, 13C NMR spectroscopy and single crystal X-ray diffraction analysis.
- Han, Hong-Fei,Guo, Zhi-Qiang,Zhang, Shao-Feng,Li, Jie,Wei, Xue-Hong
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p. 101437 - 101446
(2016)
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Read Online
- Synthesis of ent-kaurane and beyerane diterpenoids by controlled fragmentations of overbred intermediates
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Efficient access to minimally oxidized members of the ent-kaurane and beyerane class of terpenes has been achieved by using a polyene cyclization precursor designed to directly yield oxidation at the axial C19-methyl group. Construction of the [3.2.1]bicyclic system found in the ent-kaurane skeleton was realized with two overbred intermediates. Wagner-Meerwein rearrangement of the [3.2.1]bicyclic system yields the beyerane skeleton of isosteviol. Copyright
- Cherney, Emily C.,Green, Jason C.,Baran, Phil S.
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supporting information
p. 9019 - 9022
(2013/09/02)
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- IMIDE COMPLEX, METHOD FOR PRODUCING THE SAME, METAL-CONTAINING THIN FILM AND METHOD FOR PRODUCING THE SAME
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Objects of the present invention are to provide a novel niobium or tantalum complex having good vapor pressure and becoming a raw material for producing a niobium- or tantalum-containing thin film by a method such as CVD method, ALD method or the like, a method for producing the same, a metal-containing thin film using the same, and a method for producing the same. The present invention relates to producing an imide complex represented by the general formula (1) by, for example, the reaction between M1(NR1)X3(L)r (2) and an alkali metal alkoxide (3): (wherein M1 represents niobium atom or tantalum atom, R1 represents an alkyl group having from 1 to 12 carbon atoms, R2 represents an alkyl group having from 2 to 13 carbon atoms, X represents halogen atom, r is 1 when L is 1,2-dimethoxyethane ligand, r is 2 when L is pyridine ligand, and M2 represents an alkali metal), and producing a niobium- or tantalum-containing thin film by using the imide complex (1) as a raw material.
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Page/Page column 26
(2009/06/27)
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- Oxidative amination of cuprated pyrimidine and purine derivatives
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Using regioselective cuprations (via magnesiations), various primary, secondary and tertiary aminated pyrimidine and purine derivatives were prepared by the oxidative coupling of lithium amidocuprates using chloranil. DNA and RNA units such as aminated uracil or thymine, and adenine, as well as a CDK inhibitor, purvalanol A, were all obtained under mild conditions and satisfactory yields.
- Boudet, Nadege,Dubbaka, Srinivas Reddy,Knochel, Paul
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supporting information; experimental part
p. 1715 - 1718
(2009/04/10)
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- PROCESS FOE SYNTHESIZING 2-PHENYL-1H-PHENANTRHO[9,10-D]IMIDAZOLE DERIVATIVE
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The present invention describes an efficient and economical process for the preparation of a 2,3-disubstituted 2-phenyl-1h-phenantrho[9,10-d]imidazole derivative that is useful for the large scale production of material for preclinical and clinical use. The process of the present invention represents a convergent approach to generate the 2,3-disubstituted 2-phenyl-1h-phenantrho[9,10-d]imidazole derivative in high overall yield. The compound made by the process of the invention is an inhibitor of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and is therefore useful to treat pain and/or inflammation from a variety of diseases or conditions such as osteoarthritis, rheumatoid arthritis and acute or chronic pain
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Page/Page column 9
(2008/06/13)
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- 2-(PHENYL OR HETEROCYCLIC)-1H-PHENANTRHO[9,10-D]IMIDAZOLES AS MPGES-1 INHIBITORS
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The invention encompasses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful to treat pain and/or inflammation from a variety of diseases or conditions, such as osteoarthritis, rheumatoid arthritis and acute or chronic pain. Methods of treating diseases or conditions mediated by the mPGES-1 enzyme and pharmaceutical compositions are also encompassed
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Page/Page column 64-65
(2008/06/13)
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- METHODS FOR TREATING OR PREVENTING NEOPLASIAS
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The present invention is directed to a method for treating or preventing a neoplasia in a human patient in need of such treatment comprising administering to the patient a compound that inhibits microsomal prostaglandin E synthase-1 in an amount that is effective for treating or preventing the neoplasia.
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Page/Page column 67-68
(2008/06/13)
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- ARALKYL AMINES AS CANNABINOID RECEPTOR MODULATORS
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Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson’s disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, including alcohol and nicotine addiction, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.
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Page/Page column 84-85
(2010/02/11)
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- Antiviral agents
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The invention provides a compound of formula I: wherein G, R2, and R3 have any of the values defined in the specification, or a pharmaceutically acceptable salt thereof, as well as processes and intermediates useful for preparing such compounds or salts, and methods of treating a herpesvirus infection using such compounds or salts.
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- Process for the preparation of alkylamines
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Preparation of alkylamines, where, in a first process stage, an olefin is reacted with ammonia, a primary amine and/or a secondary amine under hydroaminating conditions, and then, in a second process stage, the resulting hydroamination product(s) is/are reacted under transalkylating conditions.
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- Preparation of biphosphine ligands for incorporation into catalytic complexes
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This invention relates to processes for making phosphorus compounds R2P—X—PR2, R2P—M, R2P—L and R3P, and the novel cation R2P+(L)—X—P+(L)R2, where R represents an optionally substituted hydrocarbyl group, X represents a bridging group, L represents a leaving group and M represents an alkali metal atom. The invention relates further to a process for making a compound R2P—L from a compound R—H via a new process for making the compound R—Li followed by its reaction with a compound Hal2P—L. The compound R2P—X—PR2is a ligand suitable for making catalysts for copolymerizing carbon monoxide and a olefinically unsaturated compound.
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- Mesyloxy-group migration as the stereoselective preparation method of various functionalized olefins and its reaction mechanism
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It was demonstrated that mesylation of appropriate γ,γ-difluorinated allylic alcohols under usual conditions furnished the corresponding α,γ-difluorinated allylic mesylates, possibly by way of 1,3-mesyloxy-group migration after formation of the expected "normal" intermediates, γ,γ-difluorinated allylic mesylates. This rearrangement was conveniently applied to the construction of trisubstituted allylic alcohols, α,β-unsaturated esters, amides, or ketones in good to excellent chemical yields with exclusive E selectivities.
- Yamazaki, Takashi,Hiraoka, Shuichi,Sakamoto, Johei,Kitazume, Tomoya
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p. 743 - 746
(2007/10/03)
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- Process for producing keto nitrile derivative
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A process for producing a (4S)-4-(N,N-dibenzyl)amino-5-phenyl-3-oxo-pentanenitrile derivative which comprises reacting a (2S)-2-(N,N-dibenzyl)aminophenylalanine ester derivative with acetonitrile in the presence of a lithium compound or a magnesium compound is disclosed, and a process for producing a (2S)-2-(N,N-dibenzyl)amino-5-amino-1,6-diphenyl-4-hexen-3-one derivative which comprises adding a benzylmagnesium halide or a benzyllithium to a reaction solution containing the (4S)-4-(N,N-dibenzyl)amino-5-phenyl-3-oxo-pentanenitrile derivative and reacting the derivative with the benzylmagnesium halide or the benzyllithium is also disclosed. According to these processes, optically pure (4S)-4-(N,N-dibenzyl)amino-5-phenyl-3-oxo-pentanenitrile derivative and (2S)-2-(N,N-dibenzyl)amino-5-amino-1,6-diphenyl-4-hexen-3-one derivative can be produced in a good yield on an industrial scale.
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- Homogeneous catalysts and olefin polymerization process
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Olefins are polymerized in the presence of a homogeneous catalyst represented by the formula LTi(NR2)3 wherein L is a II -bonded ligand selected from the group consisting of indenyl, C1 -C4 alkyl substituted indenyl, --OSiR3 substituted indenyl, R is a C1 -C4 alkyl group wherein each R attached to the same nitrogen atom is the same, but the R groups attached to different nitrogen atoms can be the same or different from those attached to the other nitrogen atoms.
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- BESTIMMUNG DER IONENPAAR-BASIZITAT VON LITHIUM- UND KALIUMAMIDEN
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Ion pair basicities of lithio and potassio salts of some secondary amines were determined by equilibration with benzyl compounds.With these bases it is possible to span a range of about 19 pK-units from pK = 27 up to 46.The structural dependence of thermodynamic as well as kinetic basicity is discussed.Some new effective amide bases for preparative purposes are recommended.For the first time the pK-value of toluene has been determined by direct equilibration.It amounts to 40.7 in tetrahydrofuran.
- Ahlbrecht, Hubertus,Schneider, Gunther
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p. 4729 - 4742
(2007/10/02)
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- 8α-Oestra-1,3,5(10)-triene derivatives, processes for their preparation and pharmaceutical compositions
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The invention relates to new 8α-oestra-1,3,5(10)-triene derivatives having the formula: STR1 in which R1 =H or a free, esterified or etherified hydroxy group; R2 =H or a free, esterified or etherified hydroxy group, with the proviso that at least one of the substituents R1 and R2 is different from H; R3 =alkyl (1-4 C) and R4 =O or (αX) (βY), in which X=H or aliphatic hydrocarbyl (1-4 C) and Y=a free, esterified or etherified hydroxy group and the enantiomers and racemic mixtures thereof, and also extends to processes for their preparation and to pharmaceutical compositions containing said new compounds.
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- LITHIUM DIALKYLAMIDES. 13C PARAMETERS AND SLOW PROTON TRANSFER
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The changes in 13C chemical shifts for the structural change R2NH -> R2N-Li have been measured for a series of dialkylamines.These lithiation shifts are largest at the alpha carbon (3.7-9.7 ppm) and decrease in the order α > β > χ > δ.The rates of lithium-hydrogen interchange between R2NH and R'2N-Li have been determined.The activation energies are large (9 - 17 kcal/mole) and increase as the size of R or R' increases.The slow exchange permits the direct measurement of acidity differences between pairs of amines using 13C nmr.
- Fraser, Robert R.,Baignee, Alison,Bresse, Monique,Hata, Kazumi
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p. 4195 - 4198
(2007/10/02)
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- Phenyl derivatives
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Phenyloxy, phenylsulfinyl, phenylthio, phenylsulfonyl, benzyloxy, benzylthio, benzylsulfinyl, or benzylsulfonyl, alkyl or alkenyl derivatives wherein the alkyl or alkenyl group contains at least 7 carbon atoms which are useful in killing and preventing proliferation of insects by upsetting their hormone balance.
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