- Preparation method of elviravir
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The invention provides a preparation method of elviravir, and belongs to the technical field of medicine preparation. According to the method, 2, 4-dimethoxybenzoic acid is used as a raw material and is sequentially subjected to a bromination reaction, an
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Paragraph 0087-0091
(2021/04/17)
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- Peroxidative bromination and oxygenation of organic compounds: Synthesis, X-ray crystal structure and catalytic implications of mononuclear and binuclear oxovanadium(V) complexes containing Schiffbase ligands
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Treatment of of (R,R)-N,N-salicylidene cyclohexane 1,2-diamine(H 2L1) in methanol with aqueous NH4VO3 solution in perchloric acid medium affords the mononuclear oxovanadium(V) complex [VOL1(MeOH)]·ClO4 (1) as deep blue solid while the treatment of same solution of (R,R)-N,N-salicylidene cyclohexane 1,2-diamine(H2L1) with aqueous solution of VOSO 4 leads to the formation of di-(μ-oxo) bridged vanadium(V) complex [VO2L2]2 (2) as green solid where HL 2 = (R,R)-N-salicylidene cyclohexane 1,2-diamine. The ligand HL 2 is generated in situ by the hydrolysis of one of the imine bonds of HL1 ligand during the course of formation of complex [VO 2L2]2 (2). Both the compounds have been characterized by single crystal X-ray diffraction as well as spectroscopic methods. Compounds 1 and 2 are to act as catalyst for the catalytic bromide oxidation and C-H bond oxidation in presence of hydrogen peroxide. The representative substrates 2,4-dimethoxy benzoic acid and para-hydroxy benzoic acids are brominated in presence of H2O2 and KBr in acid medium using the above compounds as catalyst. The complexes are also used as catalyst for C-H bond activation of the representative hydrocarbons toluene, ethylbenzene and cyclohexane where hydrogen peroxide acts as terminal oxidant. The yield percentage and turnover number are also quite good for the above catalytic reaction. The oxidized products of hydrocarbons have been characterized by GC Analysis while the brominated products have been characterized by 1H NMR spectroscopic studies.
- Si, Tapan Kumar,Drew, Michael G.B.,Mukherjea, Kalyan Kumar
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experimental part
p. 2286 - 2293
(2011/10/11)
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- TRIAZOLE DERIVATIVE AS AN HSP 90 INHIBITOR
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5-[4-(2-Methylphenyl)-3-hydroxy-4H-1,2,4-triazol-5-yl]-2,4-dihydroxy-N-methyl-N-butylbenzamide is an HSP90 inhibitor and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.
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Page/Page column 12
(2010/05/13)
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- Total synthesis of psoralidin, an anticancer natural product
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A base-catalyzed condensation of phenyl acetate with acid chloride, followed by intramolecular cyclization and microwave-assisted cross-metathesis reaction, leads to the first total synthesis of psoralidin, a natural product with a broad range of biological activities, in a highly convergent and regioselective manner.
- Pahari, Pallab,Rohr, Juergen
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supporting information; experimental part
p. 2750 - 2754
(2009/08/15)
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- PROCESS FOR PRODUCTION OF 4-OXOQUINOLINE COMPOUND
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The present invention provides a compound useful as a synthetic intermediate for an anti-HIV agent having an integrase inhibitory activity, a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate. Specifi
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Page/Page column 50-51
(2009/12/28)
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- METHOD FOR PRODUCING 4-OXOQUINOLINE COMPOUND
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The present invention provides a compound useful as a synthetic intermediate for an anti-HIV agent having an integrase inhibitory activity, and a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate. Spe
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Page/Page column 79
(2008/12/09)
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- TRIAZOLE DERIVATIVES
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The invention relates to novel triazole derivatives of formula (I) wherein R1 - R6 and Y have the designations cited in patent claim 1. Said derivatives are HSP90 inhibitors, and can be used to produce a medicament for treating diseases wherefore the inhibition, regulation and/or modulation of HSP90 plays an important role.
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Page/Page column 68
(2008/06/13)
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- Tetrahydronaphthyridinyl-carboxamides having anti-convulsant activity
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Compounds of formula (I) and pharmaceutically acceptable salts and solvates: where R1is hydrogen, C1-6alkyl (optionally substituted by hydroxy or C1-4alkoxy), phenyl-C1-4alkyl-, C1-6alkenyl, C1-6
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- Substituted isoquinoline derivatives and their use as anticonvulsivants
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This invention relates to novel substituted isoquinoline derivatives and their use as anticonvulsants.
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- Anti-convulsant isoquinolyl-benzamide derivatives
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Compounds of formula (I) and pharmaceutically acceptable salts thereof, where R1is hydrogen, C1-6alkyl (optionally substituted by hydroxy or C1-4alkoxy), C1-6alkenyl, C1-6alkynyl, C1-6alkylCO—, formyl, CF3CO— or C1-6alkylSO2—; R2is hydrogen or up to three substituents selected from halogen, NO2, CN, N3, CF3O—, CF3S—, CF3CO—, trifluoromethyldiazirinyl, C 1-6?alkyl, C1-6alkenyl, C1-6alkynyl, C1-6perfluoroalkyl, C3-6cycloalkyl, C3-6cycloalkyl-C1-4alkyl-, C1-6alkylO—, C1-6alkylCO—, C3-6cycloalkylO—, C3-6cycloalkylCO—, C3-6cycloalkyl-C1-4alkylO—, C3-6cycloalkyl-C1-4alkylCO—, phenyl, phenoxy, benzyloxy, benzoyl, phenyl-C1-4alkyl-, C1-6alkylS—, C1-6alkylSO2—, (C1-4alkyl)2NSO2—, (C1-4alkyl)NHSO2—, (C1-4alkyl)2NCO—, (C1-4alkyl)NHCO— or CONH2; or —NR5R6where R5is hydrogen or C1-4alkyl, and R6is hydrogen, C1-4alkyl, formyl, —CO2C1-4alkyl or —COC1-4alkyl; or two R2groups together form a carbocyclic ring that is saturated or unsaturated and unsubstituted or substituted by —OH or ═O; and the two R3groups and the two R4groups are each independently hydrogen or C1-6alkyl or the two R3groups and/or the two R4groups together form a C3-6spiroalkyl group provided that at least one R3and R4group is not hydrogen, are useful in the treatment and prophylaxis of epilepsy and other disorders.
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- N-(3-pyrrolidinyl) benzamide derivative
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N-(3-Pyrrodinyl)benzamide derivatives represented by the following general formula (I) which have potent and selective antagonism against dopamine D3 and/or D4 receptor and are useful as a psychotropic, a schizophrenia-treating agent and the like, or a pharmaceutically acceptable salt thereof or a pharmaceutical preparation thereof. STR1
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- An extended β-strand mimic for a larger artificial β-sheet
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This paper reports the development of β-strand mimic B, which duplicates the hydrogen-bonding functionality of one edge of a tetrapeptide β-strand. When attached to a tripeptide by a suitable linking group, β- strand mimic B forms a hydrogen-bonded antiparallel β-sheet structure, artificial β-sheet 2. β-Strand mimic B is based upon a 5-hydrazino-2- metboxybenzoic acid building block. The first half of the paper describes synthetic, IR and 1H NMR spectroscopic, X-ray crystallographic, and molecular modeling studies of 5-hydrazino-2-methoxybenzoic acid derivatives and related molecules. These studies establish that hydrazide derivatives of 5-hydrazino-2-methoxybenzoic acid adopt a conformation similar to that of a peptide β-strand and are suitable for use as β-strand mimics. The second half of the paper describes synthetic and 1H NMR spectroscopic studies of artificial β-sheet 2 and of controls 20 and 21, which resemble the peptidomimetic and peptide strands of 2. These experiments indicate that 2 adopts a conformation and hydrogen-bonding pattern similar to that of an antiparallel β-sheet and establish that β-strand mimic B can induce β- sheet formation in an attached peptide strand.
- Nowick, James S.,Pairish, Mason,Lee, In Quen,Holmes, Darren L.,Ziller, Joseph W.
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p. 5413 - 5424
(2007/10/03)
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- Potential antipsychotic agents. 6. Synthesis and antidopaminergic properties of substituted N-(1-benzyl-4-piperidinyl)salicylamides and related compounds. QSAR based design of more active members
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A number of substituted 2-methoxybenzamides, with and without 6-hydroxy groups, with 4-piperidinyl side-chains have been synthesized and evaluated for their antidopaminergic properties. The salicylamides were found to require a lipophilic N-substituent, like a benzyl group, for high affinity for the dopamine D-2 binding site in contrast to salicylamides with 2-pyrrolodinylmethyl side-chains. Furthermore, the influence of the aromatic substituents on the activity in the 2 series, ie 4-piperidinyl and 2-pyrrolidinylmethyl side-chains, was different. This was supported by a Hansch analysis, which could accomodate both phenolic and non-phenolic benzamides with 1-benzyl-4-piperidinyl side-chains. The activity is primarily dictated by electronic features rather than by steric and lipophilic properties. The QSAR equations were validated by the design and synthesis of a new 10-fold more active derivative. The 2 classes of benzamides with different side-chains are suggested to act on different binding sites or on different subtypes of the dopamine D-2 receptor.
- De Paulis,Hall,Kumar,Ramsby,Ogren,Hogberg
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p. 507 - 517
(2007/10/02)
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