- ISOQUINOLINE COMPOUNDS AND THEIR USE IN TREATING AhR IMBALANCE
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The present invention is directed to novel compounds of Formula (I), or a pharmaceutically acceptable salt, solvate or hydrate thereof. Pharmaceutical compositions comprising a compound of Formula (I), or a pharmaceutically acceptable salt, solvate or hydrate thereof, are also described. The invention is also directed to use of the compounds of Formula (I) for treating a condition in a mammal associated with AhR imbalance, such as an inflammatory disease or disorder.
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- Total synthesis of agastaquinone, a diterpenoid quinone isolated from Agastache rugosa
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Agastaquinone is a tricyclic diterpenoid isolated from Agastache rugose. The first total synthesis of agastaquinone was accomplished based on intramolecular Friedel-Crafts acylation of aryl lactone followed by aromatization leading to the tricyclic phenol
- Lee, Sangku,Yoo, Jisu,Jung, Jae-Kyung,Kim, Jae Nyoung,Yoon, Myeong Sik
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supporting information
p. 134 - 138
(2020/10/02)
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- SUBSTITUTED-N-HETEROARYL COMPOUNDS AND USES THEREOF
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The present disclosure relates generally to compounds useful for the treatment and/or enhancement of cognitive function and negative symptoms associated with central nervous system disorders where the circuitry involving fast spiking PV+ interneurons and the production of cortical gamma oscillations is disrupted. The subject disclosure enables the manufacture of medicaments as well as compositions containing same for use in methods of therapy and prophylaxis of cognitive dysfunction and negative symptoms.
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- Cationic Polyene Cyclization for Taiwaniaquinoid Construction
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An acid-catalyzed polyene cyclization has been used to rapidly generate the 6/5/6-fused ring system of the taiwaniaquinoid natural products. The cis-fused diastereomer was formed selectively, which enabled a step-efficient synthesis of (±)-5-epi-taiwaniaq
- Graham, Marlowe,Baker, Robert W.,McErlean, Christopher S. P.
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p. 908 - 913
(2017/02/15)
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- Efficient synthesis of sterically hindered arenes bearing acyclic secondary alkyl groups by suzuki-miyaura cross-couplings
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Bulky P,P-O ligands were designed to inhibit isomerization and reduction side reactions during the cross coupling between sterically hindered aryl halides and alkylboronic acids. Suzuki-Miyaura cross-couplings between di-ortho-substituted aryl bromides and acyclic secondary alkylboronic acids have been achieved with high yields. The method has also enabled the preparation of ortho-alkoxy di-ortho-substituted arenes bearing isopropyl groups in excellent yields. The utility of the synthetic method has been demonstrated in a late-stage modification of estrone and in the application to a new synthetic route toward gossypol. No side reaction: The shown bulky P,P-O ligands (right) successfully inhibit isomerization and reduction side reactions of the cross-coupling of sterically hindered substrates such as di-ortho-substituted aryl bromides with acyclic secondary alkylboronic acids. The method also allows the preparation of ortho-alkoxy di-ortho-substituted isopropyl arenes in excellent yields.
- Li, Chengxi,Chen, Tianyu,Li, Bowen,Xiao, Guolan,Tang, Wenjun
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supporting information
p. 3792 - 3796
(2015/03/18)
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- BORON-CONTAINING SMALL MOLECULES
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This invention provides novel compounds of the following formula and pharmaceutical compositions containing such compounds.
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- 1 -HYDROXY-BENZOOXABOROLES AS ANTIPARASITIC AGENTS
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Provided are compounds useful for controlling endoparasites both in animals and agriculture. Further provided are methods for controlling endoparasite infestations of an animal by administering an effective amount of a compound as described above, or a pharmaceutically acceptable salt thereof, to an animal, as well as formulations for controlling endoparasite infestations using the compounds described above or an acceptable salt thereof, and an acceptable carrier. The claimed compounds are described by the following Markush formula:A typical example for a compound according to above formula is: A typical example for a compound according to above formula is:
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- Enantioselective total syntheses of (-)-taiwaniaquinone H and (-)-taiwaniaquinol B by iridium-catalyzed borylation and palladium-catalyzed asymmetric α-arylation
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We report a concise, enantioselective total synthesis of (-)-taiwaniaquinone H and the first enantioselective total synthesis of (-)-taiwaniaquinol B by a route that includes asymmetric palladium-catalyzed α-arylation of a ketone with an aryl bromide that
- Liao, Xuebin,Stanley, Levi M.,Hartwig, John F.
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supporting information; experimental part
p. 2088 - 2091
(2011/04/16)
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- Approach to the synthesis of candelabrone and synthesis of 3,7-diketo-12-hydroxyabieta-8,11,13-triene
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An approach to the synthesis of aromatic diterpenes was tested for its generality.Phenylacetonitriles with increasing substitution on the aromatic ring were prepared and alkylated with geranyl bromide and the resulting dienes subjected to cationic cycliza
- Burnell, Robert H.,Caron, Stephane
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p. 1446 - 1454
(2007/10/02)
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- Synthesis of Salvilenone, a Diterpenoid Phenalenone of Salvia miltiorrhiza
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Salvilenone I, a phenalenone diterpene isolated from the roots of Salvia miltiorrhiza Bunge, was synthesized in thirteen steps from resorcinol dimethyl ether.Dihydrophenalenol derivative 19, a key intermediate, was treated with aqueous hydrobromic acid to
- Zheng, Guo-Chi,Kakisawa, Hiroshi
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p. 1117 - 1122
(2007/10/02)
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- A New General Synthetic Approach to Diterpenes: Application to Syntheses of (+ -)-Taxodione and (+ -)-Royleanone.
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High-pressure Diels - Alder reactions of 1,3,3-trimethyl-2-vinyl-1-cyclohexenes 3a,b,i with substituted 1,4-benzoquinones afford, in good yield, highly functionalized tricyclic ring systems which are found in many classes of naturally occuring terpenes.Notably, the reactions of 3a are highly regio- and stereoselective.Efficient, formal syntheses of antitumor diterpenes (+ -)-taxodione and (+ -)-royleanone are reported, which demonstrate the practical application of this new strategy for the preparation of varied terpene systems.Of particular interest is that the high-pressure reactions are accelerated by mild Lewis acids and the regio- and stereoselectivity of these reactions is also improved under the combined high-pressure / Lewis acid conditions in comparison to the high-pressure conditions alone.Indeed, in the reaction of 3a with 2-methoxy-5-methyl-1,4-benzoquinone, ZnBr2 is required to effect the Diels-Alder reaction even at 12 kbar, and endo adduct 12c is formed stereoselectively in 90percent yield.In contrast, low-temperature Ti(IV)-catalyzed reactions of diene 3a with methoxy-substituted 1,4-benzoquinones at atmospheric pressure regioselectively produce dihydrobenzofurans 19 and 20, apparently via alkylation of the quinone Ti(IV) complex by the diene followed by the ring closure.
- Engler, Thomas A.,Sampath, Umashanker,Naganathan, Sriram,Velde, David Vander,Takusagawa, Fusao
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p. 5712 - 5727
(2007/10/02)
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- Process for leukotriene antagonists
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1,3-Dialkylbenzenes are acylated and deprotected in a mixture of acetic or propionic acid and hydrobromic acid. The dihydroxyphenones thus produced are intermediates in the synthesis of leukotriene antagonists.
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