- Palladium-Catalyzed Regiospecific peri- And ortho-C-H Oxygenations of Polyaromatic Rings Mediated by Tunable Directing Groups
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An efficient divergent approach of Pd-catalyzed C-H oxygenation of polyaromatic rings is described. Reversible directing groups enable regiospecific peri- and ortho-oxygenation to readily access a wide array of polyaromatic phenols without pre- and postmanipulation of directing groups. The systematic mechanistic investigation, including deuterium-labeling experiments, palladacycle trapping, and DFT calculations, reveals that the tunable ligand-assisted C-H bond cleavage played a crucial role during the reaction process.
- Hu, Lihong,Jiang, Jing,Lin, Yaoyu,Ma, Congzhe,Song, Wanbin,Yuan, Dandan,Zhang, Yinan
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p. 279 - 284
(2021/01/13)
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- Method for preparing oxazoline insecticide arforaging intermediate
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The invention discloses a method for preparing an oxazoline insecticide arfamarin intermediate. The intermediate is 4-formyl-naphthalene-1-carboxylic acid, and compared with a synthesis route of US6613942B1, the synthesis route of the oxazoline insecticide arfamarin is simple. According to the method provided by some embodiments of the invention, through exploration, the reaction steps are shortened from three steps to one step, so the oxazoline insecticide arforlaana intermediate product with qualified purity can be obtained. The intermediate control steps are simplified, meanwhile, the product yield is increased, and industrial production is easier.
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Paragraph 0079-0085
(2021/04/21)
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- ISOXAZOLINE OXIMES AS ANTIPARASITIC AGENTS
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This invention recites naphthyl isoxazoline oxime derivatives of Formula (1) geometric isomers, stereoisomers thereof, pharmaceutically or veterinarily acceptable salts thereof, compositions thereof, and their use as a parasiticide in animals. The variables, R1a, R1b, R1c, R2, R3, and are as described herein.
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- RENIN INHIBITORS
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Disclosed are compounds of Formula (I) wherein the R, R1, R2, R3, X, Y, A, Q, E, and G are defined herein. These compounds bind to aspartic proteases to inhibit their activity and are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also disclosed are methods of use of the compounds of Formula I for ameliorating or treating aspartic protease related disorders in a subject in need thereof.
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Page/Page column 147
(2008/12/04)
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- FXR AGONISTS
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Compounds of formula wherein variables are as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating dyslipidemia and related diseases.
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Page/Page column 63
(2008/06/13)
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- AMINE COMPOUNDS AND USE THEREOF
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It is intended to provide novel amine compounds which are efficacious against diseases such as infection with HIV virus, rheumatism and cancer metastasis. Namely, amine compounds represented by the following general formula (1):In a typical case, A1 and A2 represent each an optionally substituted monocyclic or polycyclic aromatic heterocycle; W represents cyclic C3-10 alkylene, an optionally substituted monocyclic or polycyclic aromatic heterocycle, a monocyclic or polycyclic aromatic ring or a partly saturated polycyclic aromatic ring; X represents O, CH2, C(=O) or NR11; and D is a group represented by the following general formula (4) or (6).-Q-Y-BIn the formula (6), Q represents a single bond, S, O or NR12; and Y is a group represented by the following general formula (7). z represents an optionally substituted monocyclic or polycyclic aromatic ring. In the formula (6), B represents NR25R26. In the above formulae, R1 to R26 each represents hydrogen, alkyl, alkenyl or alkynyl.
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Page/Page column 55-56
(2010/02/12)
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- CXCR4-ANTAGONISTIC DRUGS COMPRISING NITROGEN-CONTAINING COMPOUND
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To provide novel nitrogen-containing compounds having antagonism to CXCR4 and remedies for disease, such as rheumatism, cancer metastasis, etc., based on the CXCR4 antagonism. Nitrogen-containing compounds represented by the following general formula and
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Page/Page column 42
(2010/02/05)
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- NITROGENOUS COMPOUNDS AND ANTIVIRAL DRUGS CONTAINING THE SAME
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The present invention provides novel compounds having antiviral activities and antiviral drugs containing the compounds as the active ingredient. The compounds are shown by the following general formula (1), wherein typically A1 and A2 are each guanidine or a group of the general fomula (ia) ; A3 is a mono- or poly-cyclic heteroaromatic ring contining 1 or 2 heteroatoms ; B1 is a single bond or alkylene group; R1 is hydrogen or alkyl group; W is an alkylene having 2-3 carbons, a cycloalkylene having 5-10 carbons, aromatic ring having 6-10 carbons, or a heteroaromatic ring having 5-10 carbons; y is C(=O)-; x is -C(=O)-NH-; n1 is an integer of 1-2; n2 is an integer of 2-3; D is a substituent selected from among various groups.
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- Synthesis and biological activity of new 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) synthase inhibitors: 2-oxetanones with a side chain mimicking the folded structure of 1233A.
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To mimic the folded side chain conformation of 1233A (1), which is a 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) synthase inhibitor, 1233A analogs with aromatic rings in the side chain were synthesized. The 2-oxetanone moiety was kept intact. Among 1233A and its synthetic analogs, trans-3-hydroxymethyl-4-[2-(7-methoxycarbonyl-1-naphthyl)ethyl]-2-oxe tanone (23) showed the highest HMG-CoA synthase inhibitory activity in vitro. The structure-activity relationship at the side chain is discussed.
- Hashizume,Ito,Yamada,Nagashima,Kanao,Tomoda,Sunazuka,Kumagai,Omura
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p. 512 - 520
(2007/10/02)
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- SUBSTITUTED IMIDAZOLES HAVING ANGIOTENSIN II RECEPTOR BLOCKING ACTIVITY
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Angiotensin II receptor antagonists having the formula: STR1 which are useful in regulating hypertension and in the treatment of congestive heart failure, renal failure, and glaucoma, pharmaceutical compositions including these antagonists, and methods of
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- Preparation of a series of substituted fluoromethylnaphthalenes
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A series of 22 3- and 4-substituted 1-fluoromethylnaphthalenes have been synthesized.Details of practical procedures for the preparation of all intermediates are described, and physical properties for all of the substituted naphthalenes synthesized, and spectral parameters for 51 previously unknown compounds, are given.
- Dixon, Elisabeth A.,Fischer, Alfred,Robinson, Frank P.
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p. 2629 - 2641
(2007/10/02)
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- Monostyryl-naphthalene derivatives
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Compounds of the formula SPC1 Wherein R' is carboxy, lower carboalkoxy or lower carboalkoxy substituted by lower dialklamino or lower trialkylammonium and Ar is phenyl substituted by cyano, carboxy or lower carboalkoxy. These compounds show a characterize
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