- De Novo Synthesis of Tricyclic 5,5-Benzannulated Spiroketals
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The synthesis of tricyclic 5,5-benzannulated spiroketal scaffolds was accomplished from 2′-hydroxyacetophenones and gem-dibromoalkenes involving a one-pot domino strategy. The hitherto unknown transformation afforded the tricyclic 5,5-benzannulated spirok
- Rao, Maddali L. N.,Islam, Sk Shamim
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- Iridium-Catalyzed C(sp3)?H Addition of Methyl Ethers across Intramolecular Carbon–Carbon Double Bonds Giving 2,3-Dihydrobenzofurans
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Intramolecular addition of an O-methyl C(sp3)?H bond across a carbon-carbon double bond occurs in the iridium-catalyzed reaction of methyl 2-(propen-2-yl)phenyl ethers. The Ir/(S)-DTBM-SEGPHOS catalyst promotes the reaction efficiently in toluene at 110–135 °C to afford 3,3-dimethyl-2,3-dihydrobenzofurans. Enantioselective C(sp3)?H addition is achieved in the reaction of methyl 2-(1-siloxyethenyl)phenyl ethers, affording enantioenriched 3-hydroxy-2,3-dihydrobenzofuran derivatives with up to 96% ee. (Figure presented.).
- Ohmura, Toshimichi,Kusaka, Satoshi,Torigoe, Takeru,Suginome, Michinori
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supporting information
p. 4448 - 4453
(2019/09/16)
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- Lithiation of a silyl ether: Formation of an ortho-fries hydroxyketone
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A hydroxy-directed alkylation of an N,N-diethylarylamide using CIPE-assisted α-silyl carbanions (CIPE=complex-induced proximity effect) has been developed using a simple reagent combination of LDA (lithium diisopropylamide) and chlorosilane. A study of the mechanism, and the application of the procedure to an anionic Snieckus-Fries rearrangement for a highly efficient synthesis of the potent phosphatidylinositol 3-kinase (PI3K) inhibitor LY294002, are reported.
- Lo, Hong-Jay,Lin, Chin-Yin,Tseng, Mei-Chun,Chein, Rong-Jie
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supporting information
p. 9026 - 9029
(2014/09/17)
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- Mono- and disalicylic acid derivatives: PTP1B inhibitors as potential anti-obesity drugs
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A series of compounds containing one or two salicylic acid moieties were synthesized, and their efficacy to inhibit the phosphohydrolase activity of PTP1B examined. Some of the methylenedisalicylic acid derivatives were potent inhibitors of PTP1B. Of those derivatives, 3c exhibited about a 14-fold selectivity against TC-PTP, and this compound was tested in a mouse model for its efficacy to prevent diet-induced obesity. It effectively suppressed the increases in body weight and adipose mass, without any noticeable toxic effect. The compound also prevented increases in the plasma triglyceride, cholesterol, and nonesterified fatty acid concentrations; thus, expanding its therapeutic potential to other related metabolic diseases, such as hyperlipidemia and hypercholesterolemia.
- Shrestha, Suja,Bhattarai, Bharat Raj,Lee, Keun-Hyeung,Cho, Hyeongjin
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p. 6535 - 6548
(2008/04/12)
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- WB4101-related compounds: New, subtype-selective α1- adrenoreceptor antagonists (or inverse agonists?)
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Our previous structure-affinity relationship study had considered the enantiomers of the naphthodioxane, tetrahydronaphthodioxane, and 2-methoxy-1-naphthoxy analogues (compounds 1, 3, and 2, respectively) of 2-(2,6-dimethoxyphenoxyethylaminomethyl)-1,4-be
- Pallavicini, Marco,Budriesi, Roberta,Fumagalli, Laura,Ioan, Pierfranco,Chiarini, Alberto,Bolchi, Cristiano,Ugenti, Maria Paola,Colleoni, Simona,Gobbi, Marco,Valoti, Ermanno
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p. 7140 - 7149
(2007/10/03)
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- (Hetero)aryl-bicyclic heteroaryl derivatives, their preparation and their use as protease inhibitors
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The present invention provides novel compounds of the Formula (I): A-B, its prodrug forms, or pharmaceutically acceptable salts thereof, wherein A represents a saturated, unsaturated, or a partially unsaturated bicyclic heterocyclic ring structure, and B represents an aryl or a heteroaryl group. Preferred compounds of the present invention comprise a benzimidazole or indole nucleus. The compounds of this invention are inhibitors of serine proteases, Urokinase (uPA), Factor Xa (FXa), and/or Factor VIIa (FVIIa), and have utility as anti cancer agents and/or as anticoagulants for the treatment or prevention of thromboembolic disorders in mammals.
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Page/Page column 65; 66
(2010/02/11)
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- PI-3 KINASE INHIBITOR PRODRUGS
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The invention provides novel prodrugs of inhibitors of PI-3 kinase. The novel compounds are LY294002 and analogs thereof comprising a reversibly quaternized amine.
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- Development of serine protease inhibitors displaying a multicentered short (<2.3 ?) hydrogen bond binding mode: Inhibitors of urokinase-type plasminogen activator and factor Xa
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Novel scaffolds that bind to serine proteases through a unique network of short hydrogen bonds to the catalytic Ser195 have been developed. The resulting potent serine protease inhibitors were designed from lead molecule 2-(2-hydroxyphenyl)1H-benzoimidazo
- Verner,Katz,Spencer,Allen,Hataye,Hruzewicz,Hui,Kolesnikov,Li,Luong,Martelli,Radika,Rai,She,Shrader,Sprengeler,Trapp,Wang,Young,Mackman
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p. 2753 - 2771
(2007/10/03)
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