- Synthesis of Novel Pterocarpen Analogues via [3?+?2] Coupling-Elimination Cascade of α,α-Dicyanoolefins with Quinone Monoimines
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By employing triethylamine as a catalyst, [3?+?2] coupling-elimination cascade of α,α-dicyanoolefins with quinone monoimines was realized. The reactions afforded various novel pterocarpen analogues with generally moderate yields (up to 75%). In addition, a plausible reaction mechanism was proposed.
- Chen, Hui,Zhao, Sihan,Cheng, Shaobing,Dai, Xingjie,Xu, Xiaoying,Yuan, Weicheng,Zhang, Xiaomei
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p. 1672 - 1683
(2019/04/08)
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- Visible-light-induced oxidation/[3 + 2] cycloaddition/oxidative aromatization to construct benzo[ a]carbazoles from 1,2,3,4-tetrahydronaphthalene and arylhydrazine hydrochlorides
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An efficient synthesis of benzo[a]carbazoles via visible-light-induced tandem oxidation/[3 + 2] cycloaddition/oxidative aromatization reactions was reported. The benzylic C(sp3)-H of tetrahydronaphthalene was activated through visible-light photoredox catalyst with oxygen as the clean oxidant under mild reaction conditions. This protocol proceeds efficiently with broad substrate scope, and the mechanism study was performed.
- Shen, Jiaxuan,Li, Nannan,Yu, Yanjiang,Ma, Chunhua
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supporting information
p. 7179 - 7183
(2019/09/30)
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- Highly enantioselective [3+2] coupling of cyclic enamides with quinone monoimines promoted by a chiral phosphoric acid
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Enantioselective [3+2] coupling of cyclic enamides with quinone monoimines was realised using a chiral phosphoric acid as a catalyst. This transformation allowed for the synthesis of highly enantioenriched polycyclic 2,3-dihydrobenzofurans (up to 99.9% ee). The absolute configuration of one product was determined by an X-ray crystal structural analysis. We also found a possible mechanism for this reaction.
- Zhang, Minmin,Yu, Shuowen,Hu, Fangzhi,Liao, Yijun,Liao, Lihua,Xu, Xiaoying,Yuan, Weicheng,Zhang, Xiaomei
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p. 8757 - 8760
(2016/07/15)
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- Efficient synthesis of 1-tetralones from 4-arylbutyric acids by combined use of solid acid catalysts and microwave irradiation
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Solid acid catalysts such as H-Beta zeolites effectively promote dehydrative intramolecular cyclization of 4-arylbutyric acids under microwave irradiation to give 1-tetralone derivatives in high yields. Copyright
- Hiroki, Kazuaki,Hatori, Makiko,Yamashita, Hiroshi,Sugiyama, Jun-Ichi
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p. 320 - 321
(2008/09/20)
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- Synthesis and structure-activity relationships of N-substituted spiropiperidines as nociceptin receptor ligands
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A series of N-substituted analogs based upon the spiropiperidine core of 1 was synthesized and exhibited high binding affinity to the nociceptin (NOP) receptor. The selectivities against other known opioid receptors were determined.
- Caldwell, John P.,Matasi, Julius J.,Zhang, Hongtao,Fawzi, Ahmad,Tulshian, Deen B.
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p. 2281 - 2284
(2007/10/03)
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- 4,5-DIHYDRONAPHTHO [1,2-b] THIOPHENE DERIVATIVE
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A 4,5-dihydronaphtho[1,2-b]thiophene derivative expressed by the formula: (wherein R1 is a C1 to C10 1-hydroxyalkyl group or a C1 to C10 acyl group, and R2 and R3 separately substitute in the 6-, 7-, 8-, or 9-positions, and are each independently a hydrogen atom, a halogen atom, a C1 to C10 alkyl group, a hydroxy group, a C1 to C10 alkoxy group, a C1 to C5 alkenyloxy group, a C1 to C5 alkynyloxy group, a benzyloxy group, or the like, provided that when R1 is an acyl group and R2 is a hydrogen atom, then R3 is neither a hydrogen atom nor an acetyl group), or a pharmaceutically acceptable salt thereof. This is a novel compound that is effective in reducing triglyceride levels in the liver and reducing blood glucose levels.
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Page/Page column 14
(2010/11/08)
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- Synthesis of 1-tetralone derivatives using a Stille cross coupling/friedel crafts acylation sequence
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An efficient method of synthesis of 1-tetralones has been achieved featuring a Stille cross-coupling reaction as the key step.
- Vercouillie, Johnny,Abarbri, Mohamed,Parrain, Jean-Luc,Duchene, Alain,Thibonnet, Jerome
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p. 3751 - 3762
(2007/10/03)
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- Synthesis of 1-tetralones by intramolecular Friedel-Crafts reaction of 4-arylbutyric acids using Lewis acid catalysts
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Intramolecular Friedel-Crafts reaction of 4-arylbutyric acids efficiently proceeded in the presence of catalytic amounts of Lewis acids such as Bi(NTf2)3 and M(OTf)3 (M=Bi, Ga, In and rare-earth metals) to form 1-tetralones. Chroman-4-one and thiochroman-4-one were also obtained in good yields from 3-phenoxypropionic acid and 3-phenylthiopropionic acid, respectively.
- Cui, Dong-Mei,Kawamura, Masato,Shimada, Shigeru,Hayashi, Teruyuki,Tanaka, Masato
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p. 4007 - 4010
(2007/10/03)
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- Bicyclic amide derivatives and their use as muscle relaxants
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Novel compounds of formula (1) together with their salts and solvates have a number of uses in medicine, in particular as central muscle relaxants.
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- Bicyclic amide derivatives and their use as muscle relaxants
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Novel compounds of formula (I) STR1 wherein R1, R2, R3 and R4 are each selected from hydrogen and fluoro and at least one and not more than two is fluoro; R5 is selected from hydrogen and C1 -C4 alkyl; R6 is selected from hydrogen, C1 -C4 ally and hydroxy; or R5 and R6 together with the ring carbon form a carbonyl group; R7 is selected from hydrogen and hydroxy, R8 and R9 are each selected from hydrogen, C1 -C4 alkyl and cyclo(C3 or C4) alkyl or together with the nitrogen form a morpholino group; and X is selected from a bond, methylene and --O-- and is always a bond or --O-- when any of R5, R6 and R7 is other than hydrogen and is always a bond when R5 and R6 together with the ring carbon form a carbonyl group; and their salts and solvates have a number of uses as central muscle relaxants. In particular, treatment of conditions associated with abnormally raised skeletal muscle tone. They are of special value in the relaxation of skeletal muscle in spastic, hypertonic and hyperkinetic conditions.
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- Amide derivatives and their therapeutic use
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Novel carbocyclic amides together with their salts, solvates and physiologically active derivatives which have a number of uses in medicine, in particular as central muscle relaxants, and in the treatment or prophylaxis of anxiety, inflammation, arthritis and pain.
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- Benzo-fused lactams that promote the release of growth hormone
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There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.
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- Synthesis of 6/7-halotetralones
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The title compounds were prepared from halobromobenzenes via a palladium catalysed coupling followed by cyclisation.
- Owton,Brunavs
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p. 981 - 987
(2007/10/02)
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- Synthesis and antiallergic activity of 2 hydroxy 3 nitro 1,4 naphthoquinones
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A selection of novel 2-hydroxy-3-nitro-1,4-naphthoquinones are shown to be potent inhibitors of rat passive cutaneous anaphylaxis (PCA) and to have highest potency with alkyl substitution at both C-6 and C-7. The most potent compounds were 7c and 7e which produced a 50% inhibition in the rat PCA test at doses of about 10 μM/kg following subcutaneous administration and showed activity after oral administration. Related 4-hydroxy-3-nitro-2(1H)-naphthalenones had no effect on rat PCA in doses up to 500 μM/kg.
- Buckle,Cantello,Smith,Spicer
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p. 1059 - 1064
(2007/10/06)
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- 2-Hydroxy-3-nitro-1,4-naphthoquinones
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Substituted naphthoquinones of the formula (I) and pharmaceutically acceptable salts thereof wherein R1, R2, R3 and R4 represent alkyl, aryl, alkoxy, hydroxy, hydrogen or halogen or any two of the groups R1, R2, R3 and R4 taken together complete a carbocyclic ring, have useful anti-allergy activity in mammals.
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