- Synthesis and reactivities of new NCN-type pincer complexes of nickel
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This report describes the preparation, characterization, and reactivities of a new family of Ni(II) complexes based on the pincer-type ligands R-NCNpz (κN,κC,κN-1,3-bis(pyrazole),5-R-C6H2; R = H, OMe). Ullman coupling of pyrazole with 1,3-diiodobenzene or 1,3-dibromo-5-methoxybenzene gave the compounds R-NC(H)Npz, which were refluxed in xylene with (i-PrCN)NiBr2 and NEt3 to give the complexes (NCNpz)NiBr (1) and (MeO-NCNpz)NiBr (2) via C-H nickelation. The aryloxide derivative (NCNpz)Ni(OAr) (3; Ar = 2,6-t-Bu2-4-Me-OC6H2) was prepared by treating the bromo precursor 1 with NaOAr, whereas the analogous reaction with NaOEt gave instead the protonated or ethoxy-functionalized ligand NC(H)Npz (major) and NC(OEt)Npz (minor). The new complexes 1-3 were fully characterized, including solid-state structures. Attempted oxidation of these complexes failed to give the target trivalent derivatives, leading instead to intractable, deeply colored Ni-containing solids, various ligand-derived side products, or an unusual I2 adduct. For example, treatment of 1 or 2 with N-bromosuccinimide gave sparingly soluble dark solids that appear to be paramagnetic, whereas 3 reacted with Br2 to give short-lived dark intermediates that decomposed over seconds to give ArOH. Reaction of the bromo complexes with aqueous H2O2 (30%) gave the functionalized ligands Br-NC(OH)Npz and NC(OH)Npz (from 1) or MeO-NC(OH)Npz (from 2), whereas 1 reacted with I2 to generate (NCNpz)NiBr·I2, an iodine adduct displaying weak Br-I interactions. Heating 1 in EtOH in air generated NC(OEt)Npz. This ligand derivatization could be extended to other alcohols (MeOH, i-PrOH, CF3CH2OH) and amines (morpholine, cyclohexylamine, aniline). Possible mechanistic scenarios for the observed oxidative, Ni-promoted Cipso-X bond formation reactions are discussed in the context of relevant literature precedents.
- Cloutier, Jean-Philippe,Vabre, Boris,Moungang-Soum, Berline,Zargarian, Davit
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Read Online
- Catalytic Formation of Coordination-Based Self-Assemblies by Halide Impurities
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The dynamics of metal organic polyhedra (MOP) play a crucial role for their application in catalysis and host-guest chemistry and as functional materials. In this contribution, we study the influence of possible contaminations of different metal precursors on the kinetic properties of MOP. Exemplary five different MOP are studied with metal precursors of varying quality. The metal precursors are either obtained from commercial sources or prepared by various literature procedures. Studies into the self-assembly process using 1H NMR and MS analyses were performed on Pt2L4, Pd2L4, Pd6L12, Pd12L24, and Ni4L6 assemblies. Commonly found impurities are shown to play a prominent role guiding selective formation of MOP, as they allow for an escape from otherwise kinetically trapped intermediates. The energy requirement for selective sphere formation is significantly lowered in many examples providing evidence for a catalytic role of halide impurities/additives in the self-assembly process. Furthermore, even though most analytical features such as 1H NMR and MS analyses show identical results for assemblies with different types of metal precursors, the dynamics of formed assemblies differs significantly if slightly less pure starting materials are used. Tiny amounts of halide contaminations make the MOP more dynamic, which can play an important role for substrate diffusion especially if bulky substrates are used. We believe that this study on the influence of impurities (which were shown to be present in some commercial sources) on the kinetic properties of MOP together with procedures of obtaining high purity metal precursors provides important information for future material preparation and provides a better understanding of already known examples.
- Bobylev, Eduard. O.,De Bruin, Bas,Reek, Joost N. H.
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Read Online
- Nickel-Catalyzed Reversible Functional Group Metathesis between Aryl Nitriles and Aryl Thioethers
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We describe a new functional group metathesis between aryl nitriles and aryl thioethers. The catalytic system nickel/dcype is essential to achieve this fully reversible transformation in good to excellent yields. Furthermore, the cyanide- and thiol-free reaction shows high functional group tolerance and great efficiency for the late-stage derivatization of commercial molecules. Finally, synthetic applications demonstrate its versatility and utility in multistep synthesis.
- Delcaillau, Tristan,Boehm, Philip,Morandi, Bill
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supporting information
p. 3723 - 3728
(2021/04/07)
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- Amphipathic rhombic supramolecular metal macrocycle as well as preparation method and application thereof (by machine translation)
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The invention discloses an amphipathic rhombic supramolecular metal macrocyclic compound as well as a preparation method and application thereof. The structure of the amphipathic rhombic supramolecular metal macrocyclic compound is shown as a formula (I). The preparation method of the amphipathic rhombic supramolecular metal macrocyclic compound comprises the following steps: mixing a glucose group-modified 120°-bipyridine ligand L and a methoxy functionalized 60°-diplatinum receptor A and the like, and forming an amphipathic rhombic supramolecular metal macrocyclic compound by self-assembly of the orientation coordinate bonds between the two Pt (II)- N. The invention further provides a preparation of the amphipathic rhombic supramolecular metal macrocyclic compound Use of a vector. (by machine translation)
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Paragraph 0052-0054; 0061-0062
(2021/01/11)
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- A containing pyrimidine group rigid conjugated macrocyclic compound and its preparation method and application (by machine translation)
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The invention relates to a containing pyrimidine group rigid conjugated macrocyclic compound and its preparation method and application, structure of the compound of the general formula: wherein n=1, 2, 3, 4, 5. The preparation comprises: to the rigid part of the 3, 5 - dibromide fluoride as the raw material for the synthesis of 3, 5 - di bromo methyl ether, then tribromide the boron escapes methylation reaction for the synthesis of 3, 5 - two-bromophenol, the linear part of the 3 - chloro - 2 - chloromethyl propylene as the starting material, to obtain the linear part of the intermediate, after 3, 5 - b bromophenol under alkaline conditions with the linear part of the intermediate synthesis of 3, 5 - b bromophenylacetic long chain ether, using 3, 5 - b bromophenylacetic long chain ethergathers two boron mellowly with dual-frequency which Miyaura reaction on synthetic monomer II; monomer II with 5 - bromo - 2 through the Suzuki coupling reaction of iodine pyrimidine synthetic monomer III; the use of monomer II and monomer III Suzuki coupling to get through. The invention the resulting compounds as functional material application. (by machine translation)
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Paragraph 0034; 0046; 0047
(2017/05/18)
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- Charge-transfer-featured materials - Promising hosts for fabrication of efficient OLEDs through triplet harvesting via triplet fusion
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A charge-transfer-featured naphthalimide derivative with a small exchange energy but a lower lying 3ππ* state than 3CT state is found to contribute to triplet harvesting through a P-type rather than an E-type delayed fluorescence, and could act as a quite promising host to achieve highly efficient OLEDs.
- Zhou, Jie,Chen, Ping,Wang, Xu,Wang, Yan,Wang, Yi,Li, Feng,Yang, Minghui,Huang, Yan,Yu, Junsheng,Lu, Zhiyun
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supporting information
p. 7586 - 7589
(2014/07/08)
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- Thiophene-coated functionalized M12L24 spheres: Synthesis, characterization, and electrochemical properties
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Instant balls: Well-defined thiophene-coated functional nanospheres were synthesized by instantaneous self-assembly of twelve 90° Pd II-containing compounds and twenty-four 120° organic bidentate ligands in acetone. This solvent system was efficient to prepare the self-assembled complexes, facilitating isolation and purification. The self-assembled functional nanospheres exhibited interesting electrochemical properties. Copyright
- Jiang, Fei,Wang, Ning,Du, Zhengkun,Wang, Jun,Lan, Zhenggang,Yang, Renqiang
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supporting information
p. 2230 - 2234,5
(2020/08/24)
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- Synthesis and pharmacological evaluation of N -(3-(1 H -Indol-4-yl)-5-(2- methoxyisonicotinoyl)phenyl)methanesulfonamide (LP-261), a potent antimitotic agent
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The synthesis and optimization of a series of orally bioavailable 1-(1H-indol-4-yl)-3,5-disubstituted benzene analogues as antimitotic agents are described. A functionalized dibromobenzene intermediate was used as a key scaffold, which when modified by sequential Suzuki coupling and Buchwald-Hartwig amination provided a flexible entry to 1,3,5-trisubstituted phenyl compounds. A 1H-indol-4-yl moiety at the 1-position was determined to be a critical feature for optimal potency. The compounds have been shown to induce cell cycle arrest at the G2/M phase and demonstrate efficacy in both cell viability and cell proliferation assays. The primary site of action for these agents is revealed by their colchicine competitive inhibition of tubulin polymerization, and a computational model has been developed for the association of these compounds to tubulin. An optimized lead LP-261 significantly inhibits growth of a human non-small-cell lung tumor (NCI-H522) in a mouse xenograft model.
- Shetty, Rupa S.,Lee, Younghee,Liu, Bin,Husain, Arifa,Joseph, Rhoda W.,Lu, Yixin,Nelson, David,Mihelcic, John,Chao, Wenchun,Moffett, Kristofer K.,Schumacher, Andreas,Flubacher, Dietmar,Stojanovic, Aleksandar,Bukhtiyarova, Marina,Williams, Ken,Lee, Kyoung-Jin,Ochman, Alexander R.,Saporito, Michael S.,Moore, William R.,Flynn, Gary A.,Dorsey, Bruce D.,Springman, Eric B.,Fujimoto, Ted,Kelly, Martha J.
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experimental part
p. 179 - 200
(2011/03/19)
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- 8-Substituted isoquinoline derivative and the use thereof
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The present invention relates to a compound represented by the following formula (1): wherein D1, A1, D2, R1, D3, and R2 each have the same meaning as defined in the present specification or a salt thereof. The compound represented by the formula (1) or a salt thereof has an IKKβ inhibiting activity and the like and is useful for the prevention and/or treatment of IKKβ-associated diseases or symptoms and the like.
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Page/Page column 240
(2010/11/03)
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- Synthesis of the tetracyclic core of tetrapetalone a enabled by a pyrrole reductive alkyation
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The tetracyclic framework of the tetrapetalone A aglycon has been secured through synthesis. A reductive pyrrole alkylation enables the formation of a key tetrasubstituted carbon stereocenter, and the tetramic acid portion of the molecule can be accessed through silicon or boronic ester conjugate addition to an ene-lactam.
- Marcus, Andrew P.,Sarpong, Richmond
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supporting information; experimental part
p. 4560 - 4563
(2010/12/25)
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- 17BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 INHIBITORS FOR THE TREATMENT OF HORMONE-RELATED DISEASES
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The invention relates to the use of non-steroidal 17beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment and prophylaxis of hormone-dependent, particularly estrogen-dependent, diseases.The invention further relates to suitable inhibitors and to a method for the production thereof.
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Page/Page column 13
(2010/08/18)
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- HETEROCYCLIC ANTIVIRAL COMPOUNDS
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Compounds of formula I, wherein R1, R2, R3, X1, X2 and Ar, are as defined herein or pharmaceutically acceptable salts thereof, inhibit HIV-1 reverse transcriptase and afford a method for prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC. The present invention also relates to compositions containing compounds of formula I useful for the prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC.
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Page/Page column 24
(2009/07/17)
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- Shape-Switchable Azo-Macrocycles
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The synthesis of four shape-switchable macrocycles comprising different peripheral substituents is described. The macro- cycles 1-4 consist of m-terphenyl semicircles interlinked by two azo joints. These macrocycles were assembled from ni- tro-functionalized m-terphenyl moieties through reductive dimerization. The semicircles were assembled through Suzuki cross-coupling reactions. The molecular weights of the macrocycles were determined by vapour pressure osmome- try, because mass spectrometry failed in the cases of 2 and 3. The E - Z photoisomerization reactions were analysed by UV/Vis spectroscopy complemented by JH NMR studies. A very slow thermal back-reaction indicated considerable stabilization of the Z isomer. The reduced efficiency of the thermal back-reaction probably arises from the reduced degree of freedom due to the mechanical interlinking of the two azo groups. The photostationary state consisted of all-Z (85%) and all-E isomers (15 %). The E - Z transformation induced by irradiation displayed simple exponential kinetics, which indicates pairwise switching of the two azo groups in a macrocycle, at least on the timescale under investigation.
- Muri, Marcel,Schuermann, Klaus C.,De Cola, Luisa,Mayor, Marcel
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experimental part
p. 2562 - 2575
(2009/09/25)
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- LEUKOTRIENE B4 INHIBITORS
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Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, COPD
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Page/Page column 55-56
(2009/09/25)
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- Non-nucleoside reverse transcriptase inhibitors
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The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein A is A1, A2, A3 or A4 and R1, R2, R3, R4a, R4b, R5, R6, Ar, X1, X2, X4, X4 and X5 are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.
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Page/Page column 22
(2008/06/13)
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- Non-nucleoside reverse transcriptase inhibitors
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Compounds of formula I, wherein R1, R2, R3, R4, Ra, X, X1, and Y are as defined herein or pharmaceutically acceptable salts thereof, inhibit HIV-1 reverse transcriptase and afford a method for prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC. The present invention also relates to compositions containing compounds of formula I useful for the prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC.
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Page/Page column 15-16
(2009/01/20)
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- Non-nucleoside reverse transcriptase inhibitors
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Compounds of formula I, wherein R1, R2, R3, R4, R5, X, Y, and Ar are as defined herein or pharmaceutically acceptable salts thereof, inhibit HIV-1 reverse transcriptase and afford a method for prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC. The present invention also relates to compositions containing compounds of formula I useful for the prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC.
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Page/Page column 20
(2008/12/08)
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- Anti-cancer agents and uses thereof
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The present invention is in the area of novel compounds and salts thereof, their syntheses, and their use as anti-cancer agents. The compounds include compounds of Formula I: and solvates, hydrates and pharmaceutically-acceptable salts thereof, wherein A1 is N or CR1; A3 is N or CR3; A5 is N or CR5; R1, R3-R6 and L are defined in the specification; n is 0 or 1; and X is an optionally-substituted aryl group having 6-10 carbons in the ring portion, an optionally-substituted 6-membered heteroaryl group having 1-3 nitrogen atoms in the ring portion, an optionally-substituted 5-membered heteroaryl group having 0-4 nitrogen atoms in the ring portion and optionally having 1 sulfur atom or 1 oxygen atom in the ring portion, or an optionally-substituted heteroaryl group in which a 6-membered ring is fused either to a 5-membered ring or to a 6-membered ring, wherein in each case 1, 2, 3 or 4 ring atoms are heteroatoms independently selected from nitrogen, oxygen and sulfur. They are effective against a broad range of cancers, especially leukemia, prostate, non-small cell lung and colon. They are additionally useful in the treatment of proliferative retinopathies such as diabetic neuropathy and macular degeneration.
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- ANTI-CANCER AGENTS ANS USES THEREOF
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The present invention is in the area of novel compounds and salts thereof, their syntheses, and their use as anti-cancer agents. The compounds include compounds of Formula (I): and solvates, hydrates and pharmaceutically-acceptable salts thereof, wherein A1 is N or CR1; A3 is N or CR3; A5 is N or CR5; R1, R3 R6 and L are defined in the specification; n is 0 or 1; and X is an optionally-substituted aryl group having 6- 10 carbons in the ring portion, an optionally-substituted 6- membered heteroaryl group having 1- 3 nitrogen atoms in the ring portion, an optionally-substituted 5- membered heteroaryl group having 0- 4 nitrogen atoms in the ring portion and optionally having 1 sulfur atom or 1 oxygen atom in the ring portion, or an optionally-substituted heteroaryl group in which a 6- membered ring is fused either to a 5- membered ring or to a 6- membered ring, wherein in each case 1, 2, 3 or 4 ring atoms are heteroatoms independently selected from nitrogen, oxygen and sulfur. They are effective against a broad range of cancers, especially leukemia, prostate, non-small cell lung and colon. They are additionally useful in the treatment of proliferative retinopathies such as diabetic neuropathy and macular degeneration.
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- Folding of coordination polymers into double-stranded helical organization
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Self-assembling coordination polymers based on PdII and Cu II metal ions were prepared from complexation of a bent-shaped bispyridine ligand and a corresponding transition metal. These coordination polymers were observed to self-assemble into supramolecular structures that differ significantly depending on the coordination geometry of the metal center. The polymer based on PdII self-assembles into a layer structure formed by bridging bispyri dine ligands connected in a trans-position of the square-planar coordination geometry of metal center. In contrast, the polymer based on CuII adopts a double-helical conformation with regular grooves, driven by interstranded, copper-chloride dimeric interaction. The double-stranded helical organization is further confirmed by structure optimization from density functional theory with aromatic framework, showing that the optimized double-helical structure is energetically favorable and consistent with the experimental results. These results demonstrate that weak metal-ligand bridging interactions can provide a useful strategy to construct stable double-stranded helical nanotubes.
- Kim, Ho-Joong,Lee, Eunji,Kim, Min Gyu,Kim, Min-Cheol,Lee, Myongsoo,Sim, Eunji
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experimental part
p. 3883 - 3888
(2009/04/17)
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- Non-nucleoside reverse transcriptase inhibitors
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The present invention provides compounds of formula I where R1 to R4 are as defined herein which are useful for treating or preventing an human immunodeficiency virus (HIV) infection, or treating AIDS or ARC. The invention further provides for methods of treating or preventing HIV infection with compounds according to formula I and compositions containing the same. The invention still further provides process for the preparation of compounds of formula I wherein R4 is A1 and X1 is NH or O.
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Page/Page column 22
(2008/06/13)
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- Non-nucleoside reverse transcriptase inhibitors
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The present invention provides for compounds useful for treating an HIV-1 infection, or preventing an HIV-1 infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein R1, R2, R3, R4, R5 and X are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds. [image]
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Page/Page column 24
(2008/06/13)
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- Heterocyclic antiviral compounds
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The present invention relates to a compounds according to formula I, methods for treating diseases mediated by human immunodeficieny virus by administration of a compound according to formula I and pharmaceutical compositions for treating diseases mediated by human immunodeficieny virus containing a compound according to formula I where R1, R2, R3, R4, R5, are as defined herein.
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Page/Page column 21-22
(2010/02/15)
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- Heterocyclic reverse transcriptase inhibitors
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The present invention provides compounds for treating or preventing an HIV infection, or treating AIDS or ARC comprising administering a compound according to formula I where R1, R2 and R3, are as defined herein.
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Page/Page column 6; 11
(2010/11/24)
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- Anti-cancer agents and uses thereof
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The present invention is in the area of novel compounds and salts thereof, their syntheses, and their use as anti-cancer agents. The compounds include compounds of Formula I: and solvates, hydrates and pharmaceutically-acceptable salts thereof, wherein A1 is N or CR1; A3 is N or CR3; A5 is N or CR5; R1, R3—R6 and L are defined in the specification; n is 0 or 1; and X is an optionally-substituted aryl group having 6-10 carbons in the ring portion, an optionally-substituted 6-membered heteroaryl group having 1-3 nitrogen atoms in the ring portion, an optionally-substituted 5-membered heteroaryl group having 0-4 nitrogen atoms in the ring portion and optionally having 1 sulfur atom or 1 oxygen atom in the ring portion, or an optionally-substituted heteroaryl group in which a 6-membered ring is fused either to a 5-membered ring or to a 6-membered ring, wherein in each case 1, 2, 3 or 4 ring atoms are heteroatoms independently selected from nitrogen, oxygen and sulfur. They are effective against a broad range of cancers, especially leukemia, non-small cell lung and colon.
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Page/Page column 35
(2008/06/13)
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- Pyrazole derivatives
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This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivative thereof, wherein R1 to R4 are defined in the description, and to processes for the preparation thereof, intermediates used in their preparation of, compositions containing them and the uses of such derivatives. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof. As such the compounds of the present invention are useful in the treatment of a variety of disorders including those in which the inhibition of reverse transcriptase is implicated. Disorders of interest include those caused by Human Immunodificiency Virus (HIV) and genetically related retroviruses, such as Acquired Immune Deficiency Syndrome (AIDS).
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Page/Page column 11
(2010/02/11)
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- PYRAZOLE DERIVATIVES AS REVERSE TRANSCRIPTASE INHIBITORS
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This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivative thereof, wherein R' to R4 are defined in the description, and to processes for the preparation thereof, intermediates used in their preparation of, compositions containing them and the uses of such derivatives. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof. As such the compounds of the present invention are useful in the treatment of a variety of disorders including those in which the inhibition of reverse transcriptase is implicated. Disorders of interest include those caused by Human Immunodificiency Virus (HIV) and genetically related retroviruses, such as Acquired Immune Deficiency Syndrome (AIDS)
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- PYRAZOLE DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS FOR HIV MEDIATED DISEASES
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This invention relates to pyrazole derivatives of formula (I)or pharmaceutically acceptable salts, solvates or derivative thereof, wherein R' to R4; ;ark defined in the description, and to processes for the preparation thereof, intermediates used in their preparation of, compositions containing them and the uses of such derivatives. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof. As such the compounds of the present invention are useful in the treatment of a variety of disorders including those in which the inhibition' of reverse transcriptase is implicated. Disorders of interest include those caused by Human Immunodificiency Virus (HIV) and genetically related retroviruses, such as Acquired Immune Deficiency Syndrome (AIDS).
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- 4-(3,5-DICYANOPHENOXY) PYRAZOLE DERIVATIVES FOR USE AS TRANSCRIPTASE MODULATORS IN THE TREATMENT OF I.A. HIV
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This invention relates to the pyrazole derivatives of formula (I) and pharmaceutically acceptable salt, solvate or derivatives thereof, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. The compounds of the invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors, thereof. Reverse transcriptase is implicated in the infectious lifecycle of Human Immunodeficiency Virus (HIV). Compounds which interfere with the function of this enzyme have shown utility in the treatment of conditions caused by HIV and genetically related retroviruses, such as Acquired Immune Deficiency Syndrome (AIDS).
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Page/Page column 18
(2010/02/06)
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- PYRAZOLE DERIVATIVES
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This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivative thereof, wherein R1 to R4, n W, X and Y are defined in the description, and to processes for the preparation thereof, intermediates used in their preparation of, compositions containing them and the uses of such derivatives. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof. As such the compounds of the present invention are useful in the treatment of a variety of disorders including those in which the inhibition of reverse transcriptase is implicated. Disorders of interest include those caused by Human Immunodificiency Virus (HIV) and genetically related retroviruses, such as Acquired Immune Deficiency Syndrome (AIDS).
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- PYRAZOLE AMIDES FOR TREATING HIV INFECTIONS
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This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivative thereof, wherein R' to R4, n W, X and Y are defined in the description, and to processes for the preparation thereof, intermediates used in their preparation of, compositions containing them and the uses of such derivatives. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof. As such the compounds of the present invention are useful ín the treatment of a variety of disorders including those in which the inhibition of reverse transcriptase is implicated. Disorders of interest include those caused by Human Immunodificiency Virus (HIV) and genetically related retroviruses, such as Acquired Immune Deficiency Syndrome (AIDS).
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- Expedient total syntheses of rhein and diacerhein via fries rearrangement
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Short and practical total syntheses of rhein (1) and diacerhein (2) have been achieved via a Fries rearrangement and bis-carbonylation strategy followed by cyclization in molten salt, starting from dibromoester 7.
- Tisserand, Steve,Baati, Rachid,Nicolas, Marc,Mioskowski, Charles
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p. 8982 - 8983
(2007/10/03)
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- Pyrazole derivatives
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This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivatives thereof, and to processes for the preparation thereof, intermediates used in their preparation of, compositions containing them and the uses of such derivatives. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof. As such, the compounds of the present invention are useful in the treatment of a variety of disorders including those in which the inhibition of reverse transcriptase is implicated. Disorders of interest include those caused by Human Immunodificiency Virus (HIV) and genetically related retroviruses, such as Acquired Immune Deficiency Syndrome (AIDS).
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- Selective lithiation of phloroglucinol mixed alkyl ethers. The synthesis of pseudoaspidinol-B
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The title reaction is regioselective with the methyl di-t-butyl ether (4) but not with the di-i-propyl analogue (3).
- Halonen, Aija,Hase, Tapio A.
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p. 7327 - 7328
(2007/10/02)
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- POLYBROMINATED AROMATIC COMPOUNDS. IV. METHOXYDEBROMINATION REACTIONS OF POLYBROMOBENZENES IN PYRIDINE
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The rates were measured and the orientation was studied for the methoxydebromination of all polybromobenzenes C6HnBr6-n (n = 0-3) in pyridine at 115 deg C.From comparison of the partial rates of substitution of the bromine atom at various positions of the benzene ring it was found that the activating effect of the bromine atom in relation to the point of nucleophilic attack changes in the order o-Br > m-Br > p-Br, and the directing selectivity of the bromine is low (compared with fluorine in the methoxydefluorination of polyfluorobenzenes) and increases with decrease in the number of bromine atoms in the aromatic ring of the substrate.
- Shishkin, V. N.,Lapin, K. K.,Tanaseichuk, B. S.,Butin, K. P.
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p. 516 - 522
(2007/10/02)
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- POLYBROMINATED AROMATIC COMPOUNDS. III. SYNTHESIS OF BROMINE-SUBSTITUTED ANISOLES
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Reliable methods were developed for the synthesis of di-, tri-, and tetrabromoanisoles, and all the possible individual isomers were synthesized.The structures of the isomers were proved by alternative synthesis and spectral methods (PMR, IR).It was shown that the published data are incorrect in a number of cases; either the final product was assigned the incorrect structure, or the published methods led to mixture of the various isomers.
- Shishkin, V. N.,Tanaseichuk, B. S.,Lapin, K. K.,Ivkina, A. A.,Butin, K. P.
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p. 2357 - 2366
(2007/10/02)
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