- Practical Method for the Synthesis and Optical Resolution of Axially Dissymmetric 6,6'-Dimethylbiphenyl-2,2'-dicarboxylic Acid
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Racemic 6,6'-dimethylbiphenyl-2,2'-dicarboxylic acid (1) could be conveniently synthesized and efficiently resolved by the recrystallization of the brucine salts in satisfactory yields.Each enantiomer, thus obtained, was confirmed to be optically pure from a high-performance liquid chromatographic (HPLC) analysis on an optically active column.
- Kanoh, Shigeyoshi,Muramoto, Hiroki,Kobayashi, Natsumi,Motoi, Masatoshi,Suda, Hiroshi
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- A Fullerene-Based Molecular Torsion Balance for Investigating Noncovalent Interactions at the C60 Surface
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To investigate the nature and strength of noncovalent interactions at the fullerene surface, molecular torsion balances consisting of C60 and organic moieties connected through a biphenyl linkage were synthesized. NMR and computational studies
- Maeda, Yutaka,Narita, Haruna,Yamada, Michio
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- A significant improvement in enantioselectivity, yield, and reactivity for the copper-bi-o-tolyl bisoxazoline-catalyzed asymmetric allylic oxidation of cyclic olefins using recoverable SBA-15 mesoporous silica material
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A series of chiral bi-o-tolyl bisoxazoline ligands 1 and 2 were conveniently synthesized on a gram scale from inexpensive and commercially available 3-methyl benzoic acid in eight steps. The catalytic and induced asymmetric effects of the chiral copper (I) complexes of these ligands on the asymmetric allylic oxidation of cycloolefins were investigated in the presence of various nano-sized additives. When SBA-15 mesoporous silica was used in conjunction with these ligands very highly enantioselectivities (up to 97% ee) and excellent yields (up to 99%) of the corresponding chiral allylic esters were obtained in a reasonably short period of time.
- Samadi, Saadi,Nazari, Saber,Arvinnezhad, Hamid,Jadidi, Khosrow,Notash, Behrouz
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- Asymmetric allylic oxidation with biarylbisoxazoline-copper(I) catalysis
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Eight new bi-o-tolyl bisoxazolines were made and used as ligands in the copper catalyzed asymmetric allylic oxidation reaction. Three benzoyl tert-butyl peresters, p-nitro, o-iodo, and 2,4,6-trichloro were made and used with cyclohexene and cyclopentene w
- Andrus, Merritt B,Asgari, Davoud
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- Divergent syntheses of iodinated isobenzofuranones and isochromenones by iodolactonization of 2-alkynylbenzoic acids in ionic liquids
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The regiochemical outcome of the iodolactonization of 2-alkynylbenzoic acids, carried out at 100 °C in ionic liquids (ILs) as unconventional solvents and with molecular iodine as the iodine source, in the absence of external bases, was found to be strongl
- Mancuso, Raffaella,Pomelli, Christian C.,Malafronte, Francesco,Maner, Asif,Marino, Nadia,Chiappe, Cinzia,Gabriele, Bartolo
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supporting information
p. 4831 - 4841
(2017/07/10)
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- CHEMICAL COMPOUNDS
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The invention relates to a novel compound of formula (I) or a stereoisomer, or a racemate or a mixture or a pharmaceutically acceptable salt thereof: wherein: R is phenyl or a 5- or 6-membered heteroaryl ring containing 1 to 3 heteroatoms selected from S, N and O, such rings may be optionally substituted with n groups Q; Q is selected from a group consisting of: C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN, SO2CH3 or a group —O[(CR1R2]pQ1; or Q may be a group Q2; Q1 is phenyl, which may be optionally substituted with n substituents selected from a group consisting of: C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN, or a group Q2; or corresponds to 2,2-difluoro-benzo[d][1,3]dioxol-4-yl; Q2 is a 5- or 6-membered heteroaryl containing at least one nitrogen atom, which may optionally substituted with n substituents selected from a group consisting of: Cl C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN; P is a 6-membered heteroaryl or a 8-1 1 membered bicyclic heteroaryl group, which may be substituted with n substituents selected from a group consisting of: C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN; R1 is hydrogen or C1-C3 alkyl; R2 is hydrogen or C1-C3 alkyl; n is 1, 2 or 3; p is 0, 1 or 2; and with the proviso that when R corresponds to phenyl, P is substituted by at least one CF3; processes for the preparation of those compounds, pharmaceutical compositions containing one or more compounds of formula (I) and their use as dual antagonists of the Orexin 1 and Orexin 2 receptors.
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Paragraph 0204; 0205; 0206
(2014/12/09)
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- CHEMICAL COMPOUNDS
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The invention relates to a novel compound of formula (I) or a stereoisomer, or a racemate or a mixture or a pharmaceutically acceptable salt thereof: wherein: R is phenyl or a 5- or 6-membered heteroaryl ring containing 1 to 3 heteroatoms selected from S, N and O, such rings may be optionally substituted with n groups Q; Q is selected from a group consisting of: C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN, SO2CH3 or a group -O[(CR1R2]pQ1; or Q may be a group Q2; Q1 is phenyl, which may be optionally substituted with n substituents selected from a group consisting of: C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN, or a group Q2; or corresponds to 2,2-difluoro- benzo[d][1,3]dioxol-4-yl; Q2 is a 5- or 6-membered heteroaryl containing at least one nitrogen atom, which may optionally substituted with n substituents selected from a group consisting of: C1 C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN; P is a 6-membered heteroaryl or a 8-1 1 membered bicylic heteroaryl group, which may be substituted with n substituents selected from a group consisting of: C1-C4 alkyl, halogen, halo C1-C4 alkyl, C1-C4 alkoxy, CN; R1 is hydrogen or C1-C3 alkyl; R2 is hydrogen or C1-C3 alkyl; n is 1, 2 or 3; p is 0, 1 or 2; and with the proviso that when R corresponds to phenyl, P is substituted by at least one CF3; processes for the preparation of those compounds, pharmaceutical compositions containing one or more compounds of formula (I) and their use as dual antagonists of the Orexin 1 and Orexin 2 receptors.
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Page/Page column 36; 37
(2013/07/05)
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- Design, synthesis and identification of novel colchicine-derived immunosuppressant
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Synthesis and biological evaluation of various colchicine analogues through the mixed-lymphocyte reaction (MLR), lymphoproliferation, and inhibitory effects on the inflammatory genes are described. In addition, a new series of immunosuppressive agents developed on the structural basis of colchicine, as well as their structure-activity relationships is reported. The most potent analogue 20a exhibited an excellent immunosuppressive activity on in vivo skin-allograft model, which is comparable to that of cyclosporin A.
- Chang, Dong-Jo,Yoon, Eun-Young,Lee, Geon-Bong,Kim, Soon-Ok,Kim, Wan-Joo,Kim, Young-Myeong,Jung, Jong-Wha,An, Hongchan,Suh, Young-Ger
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scheme or table
p. 4416 - 4420
(2010/04/05)
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- ADAMANTYL DERIVATES AS P2X7 RECEPTOR ANTAGONISTS
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The invention provides compounds of formula (I) pharmaceutically acceptable salt or solvate thereof, in which R1, A1, m and A are as defined in the specification; a process for their preparation; pharmaceutical compositions containin
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Page/Page column 72-73
(2010/10/20)
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- Synthesis, Resolution, and Applications of 1,16-Dihydroxytetraphenylene as a Novel Building Block in Molecular Recognition and Assembly
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This paper concerns the synthesis of 1,16-dihydroxytetraphenylene (DHTP) (2) by employing a novel NBS bromination route. (±)-DHTP 2 was successfully resolved into its optical antipodes and converted to (±)-1,16-bis(diphenylphosphino)tetraphenylene (BPTP) (26), whose platinum complex BPTP-PtCl2 (27) was also obtained. As a hydrogen bond donor, racemic and optically active DHTP 2 was allowed to assemble with 4,4′-bipyridine to form single crystals of good quality. X-ray Diffraction studies of these crystals revealed that the crystallographic packing of the hydrogen bonded complex between (±)-2 and 4,4′-bipyridine was different from the one formed from (S)-2 and 4,4′-bipyridine. It was found that an infinite zigzag chain with alternate chirality was formed in the assembly of (±)-2 and 4,4′-bipyridine, while (S)-2 and 4,4′-bipyridine failed to show the same assembly pattern. The reason (±)-2 formed an alternate and zigzag chain with 4,4′-bipyridine was most likely due to the inherent stability of this supramolecular assembly. The chiral recognition between 2 and optically active BINAP under the direction of platinum(II) has also been examined. 1H and 31P NMR spectroscopic studies demonstrated that there was an obvious discrimination of 2 between the enantiomers of BINAP-PtCO3.
- Wen, Jian-Feng,Hong, Wei,Yuan, Ke,Mak, Thomas C. W.,Wong, Henry N. C.
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p. 8918 - 8931
(2007/10/03)
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