31202-23-0Relevant articles and documents
O-arylation versus C-arylation: Copper-catalyzed intramolecular coupling of aryl bromides with 1,3-dicarbonyls
Fang, Yewen,Li, Chaozhong
, p. 6427 - 6431 (2006)
The copper-catalyzed intramolecular coupling of aryl bromides with 1,3-dicarbonyls via a six-membered ring closure was examined. With CuI (10 mol %) as the catalyst, N,N′-dimethylethylenediamine as the ligand, and Cs2CO3 as the base,
Selective synthesis of 1-, and 3-carbomethoxy 2-tetralol stereoisomers by microbial reduction of the corresponding tetralones
Abalain, Cecile,Buisson, Didier,Azerad, Robert
, p. 2983 - 2996 (1996)
The microbial reduction of β-ketoesters derived from 2-tetralone has been shown to produce good yields of 2-hydroxy-1-carboxy- or 3-hydroxy-2-carboxyesters. Baker's yeast invariably affords a high enantiomeric purity cis-hydroxyester, while fungi strains may produce, sometimes exclusively, cis- or trans- complementary stereochemistries. From a general survey of the baker's yeast reduction of cyclic β-ketoesters, a working model for predicting enantio- and diastereoselectivities of the reduction is proposed and discussed.
2,4-Diaminopyrimidines as dual ligands at the histamine H1 and H4 receptor - H1/H4-receptor selectivity
Hammer, Sebastian G.,Gobleder, Susanne,Naporra, Franziska,Wittmann, Hans-Joachim,Elz, Sigurd,Heinrich, Markus R.,Strasser, Andrea
supporting information, p. 292 - 300 (2016/01/09)
Distinct diaminopyrimidines, for example, 4-(4-methylpiperazin-1-yl)-5,6-dihydrobenzo[h]quinazolin-2-amine are histamine H4 receptor (H4R) antagonists and show high affinity to the H4R, but only a moderate affinity to the
Mechanistic studies on the CAN-mediated intramolecular cyclization of δ-aryl-β-dicarbonyl compounds
Casey, Brian M.,Sadasivam, Dhandapani V.,Flowers II, Robert A.
, p. 1472 - 1479 (2013/08/23)
The synthesis of 2-tetralones through the cyclization of δ-aryl-β-dicarbonyl substrates by using CAN is described. Appropriately functionalized aromatic substrates undergo intramolecular cyclizations generating 2-tetralone derivatives in moderate to good yields. DFT computational studies indicate that successful formation of 2-tetralones from δ-aryl-β-dicarbonyl radicals is dependent on the stability of the subsequent cyclohexadienyl radical intermediates. Furthermore, DFT computational studies were used to rationalize the observed site selectivity in the 2-tetralone products.
Palladium catalysed bis- and tris-cyclisations furnishing fused cyclopropyl carbo/heterocycles
Grigg, Ronald,Sakee, Uthai,Sridharan, Visuvanathar,Sukirthalingam, Sukanthini,Thangavelauthum, Ravishanker
, p. 9523 - 9532 (2007/10/03)
Catalytic bis- and tris-cyclisation of a series of acyclic carbo- and heterocyclic precursors results in formation of two or three rings, two or three C-C bonds and two asymmetric tetrasubstituted C-centres regio- and stereoselectively in excellent yield.
2-Amino-1-functionalized tetralin derivatives and related glycogen phosphorylase inhibitors
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Page/Page column 17, (2008/06/13)
Novel compounds are provided which are glycogen phosphorylase inhibitors which are useful in treating, preventing or slowing the progression of diseases requiring glycogen phosphorylase inhibitor therapy such as diabetes and related conditions (such as hy
cis- and trans-N-benzyl-octahydrobenzo[g]quinolines. Adrenergic and dopaminergic activity studies
Thermos, Kyriaki,Froudakis, George E.,Tagmatarchis, Nikos,Katerinopoulos, Haralambos E
, p. 883 - 886 (2007/10/03)
In vitro assays on a series of cis- and trans-octahydrobenzo[g]quinolines indicated an unusual trend of affinities at the dopaminergic receptors and α adrenoceptors. The trans N-benzyl analogues exhibited affinity at the α2 as well as the D1-like receptors whereas their N-unsubstituted congeners showed a distinct preference for the α2 adrenoceptor. Enhanced activity for the α2 receptors was also exhibited by the cis N-benzylated isomers. These observations are interpreted by theoretical calculations.
Asymmetric palladium annulation: Formal synthesis of (+)-huperzine A
Chassaing, Christophe,Haudrechy, Arnaud,Langlois, Yves
, p. 8805 - 8809 (2007/10/03)
A new formal stereoselective synthesis of (+)-huperzine A 1 was achieved using as a key step a palladium mediated annulation between 2-methylene-1,3- propanediol diacetate and (1R,2S)-2-phenylcyclohexanol derived β-ketoester 14.
A diastereoselective synthesis of trans/cis octahydronaphthoquinolizine
Kouvarakis,Katerinopoulos
, p. 3035 - 3044 (2007/10/03)
The tetracyclic system of 2,3,6,7,7a,8,12b,12c-octahydro-1H,5H-naphtho[1,2,3,i,j]quinolizine with trans/cis fusions of the B/D and B/C rings has been diastereospecifically synthesized in nine steps and in 23% total yield.