- Total Synthesis of (-)-N-Methylwelwitindolinone C Isothiocyanate Based on a Pd-Catalyzed Tandem Enolate Coupling Strategy
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The highly stereocontrolled total synthesis of (-)-N-methylwelwitindolinone C isothiocyanate is described, which features the expeditious construction of a bicyclo[4.3.1]decane ring system by a palladium-catalyzed tandem enolate allylation/arylation reaction.
- Komine, Keita,Nomura, Yusuke,Ishihara, Jun,Hatakeyama, Susumi
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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 9; 12; 13-14; 15-18; 19-20; 24; 25
(2009/06/27)
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- Synthesis of beta-elemene, intermediates thereto, analogues and uses thereof
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The present invention provides convergent processes for preparing beta-elemene, and analogues thereof. Also provided are analogues related to beta-elemene and intermediates useful for preparing the same. The present invention further provides novel compositions based on analogues of beta-elemene and methods for the treatment of cancer, such as brain tumor, lung cancer, colorectal cancer, gastric intestional cancer, and stomach cancer.
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Page/Page column 11
(2010/02/15)
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- METHOD FOR PRODUCING AN OPTICALLY ACTIVE TETRAHYDROQUINOLINE
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The present invention provides an industrially advantageous production method of optically active tetrahydroquinolines of formula (1), which comprises: 1) a step of reacting a β-ketoester of formula (2) with an amine of formula (3) to produce an enaminoester of formula (4); 2) a step of subjecting the enaminoester of formula (4) above obtained in 1) to asymmetric hydrogenation to produce an optically active β-amino acid derivative of formula (5); 3) a step of amidating the optically active β-amino acid derivative (5) above obtained in 2) to produce an amide of formula (6); 4) step of alkoxycarbonylating the amide of formula (6) above obtained in 3) to produce a compound of formula (7); and 5) a step of subjecting the compound of formula (7) above to cyclization to produce the optically active tetrahydroquinoline of formula (1).
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- Oxazolidinone derivatives with antibiotic activity
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Compounds of the formula (I), or a pharmaceutically acceptable salt, or an in-vivo-hydrolysable ester thereof, wherein HET is an N-linked 5-membered heteroaryl ring, optionally substituted on a C atom by an oxo or thioxo group; and/or by 1 or 2 (1-4C)alkyl groups; and/or on an available nitrogen atom by (1-4C)alkyl; or HET is an N-linked 6-membered heteroaryl ring containing up to three nitrogen heteroatoms in total, optionally substituted on a C atom as above; Q is selected from, for example, Q1 R2 and R3 are independently hydrogen or fluoro; T is selected from a range of groups, for example, of formula (TC5) wherein Rc is, for example, R13CO—, R13SO2— or R13CS—; wherein R13 is, for example, optionally substituted (1-10C)alkyl or R14C(O)O(1-6C)alkyl wherein R14 is optionally substituted (1-10C)alkyl; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are described.
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Page/Page column 33
(2010/11/30)
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- CYCLOPROPYL CONTAINING OXAZOLIDINONE ANTIBIOTICS AND DERIVATIVES THEREOF
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This invention relates to new oxazolidinones having a cyclopropyl moiety, which are effective against aerobic and anerobic pathogens such as multi-resistant staphylococci, streptococci and enterococci, Bacteroides spp., Clostridia spp. species, as well as acid-fast organisms such as Mycobacterium tuberculosis and other mycobacterial species. The compounds are represented by structural formula I: 1its enantiomer, diastereomer, or pharmaceutically acceptable salt or ester thereof.
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- Oxazolidinones to treat eye infections
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The present invention involves a method of treating an ophthalmic infection in a useful warm blooded mammal who is in need of such treatment which comprises topical administration of an ophthalmologically effective amount of an OXAZOLIDINONE.
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- Piperazinonephenyloxazolidinone derivatives and their use as antibacterial agents
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PCT No. PCT/GB97/00169 Sec. 371 Date Jul. 27, 1998 Sec. 102(e) Date Jul. 27, 1998 PCT Filed Jan. 21, 1997 PCT Pub. No. WO97/27188 PCT Pub. Date Jul. 31, 1997The invention concerns a compound of formula (I) wherein: R1 is of the formula -NHC(=O)(1-4C)alkyl, -NHS(O)n(1-4C)alkyl wherein n is 0, 1 or 2 or R1 is hydroxy; R2 and R3 are independently hydrogen or fluoro; R4 is hydrogen, methyl, ethyl or oxo; R5 is hydrogen, (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl or of the formula R6(CH2)m- wherein either m is 1-4 and R6 is, for example, trifluoromethyl, difluoromethyl, fluoromethyl, (1-4C)alkoxy, (1-4C)alkyl S(O)p- wherein p is 0, 1 or 2, (1-6C)alkanoyloxy, di-(+E,uns N+EE -(1-4C)alkyl)amino, +E,uns N+EE -((1-4C)alkyl)(1-4C)alkanoylamino, cyano, carboxy, (1-4C)alkoxycarbonyl, carbamoyl, di-(+E,uns N+EE -(1-4C)alkyl)carbamoyl, +E,uns N+EE -((1-4C)alkyl)(1-4C)alkanesulphonamido, +E,uns N+EE 1-((1-4C)alkyl)-di-(+E,uns N+EE 3-(1-4C)alkyl)ureido, or of the formula -OC(=O)NR7(R8) or -N(R9)SO2NR7(R8) wherein R7 and R8 are independently hydrogen or (1-4C)alkyl and R9 is (1-4C)alkyl; or m is 2-4 and R6 is, for example, hydroxy, (1-4C)alkanoylamino, amino, (1-4C)alkylamino, (1-4C)alkanesulphonamido, ureido, di-(+E,uns N+EE 3-(1-4C)alkyl)ureido or of the formula -NHSO2NR7(R8); and pharmaceutically-acceptable salts thereof; processes for their preparation; pharmaceutical compositions containing them and their use as antibacterial agents.
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- Preparation of lithium alkoxides
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A process for producing clear, colorless solutions of branched lithium alkoxides containing 3 to 12 carbon atoms, in a polar reaction solvent, comprising reacting a dispersion of lithium metal having a particle size less than 300 microns with a minimum of 5 mole percent excess over stoichiometric of a branched alkyl alcohol containing 4 to 12 carbon atoms, in a polar reaction solvent as the reaction medium, at a temperature between 50° C. and the boiling point of the solvent in an inert atmosphere.
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- Proton affinities and aggregation states of lithium alkoxides, phenolates, enolates, β-dicarbonyl enolates, carboxylates, and amidates in tetrahydrofuran
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The proton affinities of the title compounds are represented by their heats of deprotonation, ΔHdep, through reactions with lithium bis(trimethylsilyl)amide, LiHMDS, in tetrahydrofuran at 25°C. Aggregation numbers of the parent acid and of its lithium salt at a concentration of 0.10 M were obtained by vapor-pressure osmometry at 37°C. Lithium phenolates were also studied by conductivity at 25°C. ΔHdeps for 27 oxygen, nitrogen, and carbon acids of varied types correlate fairly well (R = 0.95) with their published pKas in dimethyl sulfoxide although their degrees of aggregation in THF vary from one to over seven. In some cases, the ΔHdep of an acid is strongly dependent on the concentration ratio of LiHMDS to that of the acid's lithium salt at the time of measurement. Aggregation numbers determined by VPO in this report agree with available published values obtained by previous workers using several techniques. There is no obvious relationship between the aggregation number of the lithium salt and the basicity of the corresponding anion as represented by ΔHdep. This observation along with independent evidence for equilibria between monomers, dimers, tetramers, etc. for a number of compounds indicate that there are only small differences between the relative stabilities of different aggregation states. Conductance data for lithium p-nitrophenolate were treated by Wooster analysis, the results of which suggest equilibria between ion triplets, ion pairs, and free ions in THF. The conductance of LiHMDS in this solvent is surprisingly high, and this property was used to demonstrate an interaction between LiHMDS and lithium o-tert-butylphenolate.
- Arnett, Edward M.,Moe, Kevin D.
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p. 7288 - 7293
(2007/10/02)
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- SYNTHESIS OF 3,6-DISUBSTITUTED &β-CARBOLINES WHICH POSSESS EITHER BENZODIAZEPINE ANTAGONIST OR AGONIST ACTIVITY
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A series of 3-substituted and 3,6-disubstituted β-carbolines have been synthesized.These compounds have been screened in vitro in order to determine the size of substituents which benzodiazepine receptors will tolerate at positions -3 and -6 of the β-carboline nucleus.It has been found that the receptor will tolerate ester alkyl groups at position-3 as large as cyclohexyl 1g but not as large as adamantyl 5d.Moreover, N-aryl substituents as large as naphthobenzylamino 8b can be introduced at position-6 without significant loss of receptor binding affinity.
- Hagen, Timothy J.,Guzman, Filadelfo,Schultz, Christopher,Cook, James M.,Skolnick, Phil,Shannon, Harlan E.
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p. 2845 - 2855
(2007/10/02)
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- EVIDENCE FOR SINGLE ELECTRON TRANSFER IN THE REACTION OF ALKOXIDES WITH ALKYL HALIDES
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Evidence for a radical process in the reaction of lithium alkoxides with alkyl iodides was obtained by observation of cyclization of appropriate radical probes, by the trapping of radicals, and by EPR spectroscopic observations relating to the one electron donor properties of alkoxides.
- Ashby, E. C.,Bae, Dong-Hak,Park, Won-Suh,Depriest, Robert N.,Su, Wei-Yang
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p. 5107 - 5110
(2007/10/02)
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- Process for introducing alkyl radicals into carbon chains having a functional group and compounds prepared by said process
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Process for introducing a substituent selected from branched- or straight-chain alkyl radicals having from 1 to 12 carbon atoms, aralkyl or cycloalkyl radicals in which the alkyl moiety has from 1 to 4 carbon atoms, into a carbon chain bearing a stable functional group the said carbon chain having at least one proton in α-position in relation to this functional group, process whereby, in a first step, this carbon chain is reacted with a complex base comprising a mixture of alkali metal amide and alkali metal alcoholate suspended in an anhydrous organic solvent to provide temporarily a carbanion, then in a second step this carbanion is reacted in an anhydrous organic solvent with an alkyl, aralkyl or cycloalkyl halide corresponding to the substituent to be introduced.
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