- Synthesis and appetite suppressant activity of 1-aryloxy-2-substituted aminomethyltetrahydronaphthalenes as conformationally rigid analogues of fluoxetine
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Several 1-aryloxy-2-substituted aminomethyltetrahydronaphthalenes (7-21) as conformationally rigid analogues of fluoxetine were synthesized and evaluated for their anorexigenic and antidepressant activities. For SAR studies the related acyclic analogues (
- Bhandari, Kalpana,Srivastava, Shipra,Shankar, Girija,Nath, Chandishwar
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p. 2535 - 2544
(2007/10/03)
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- Further exploration of 1-{2-[Bis-(4-fluorophenyl)methoxy]ethyl}piperazine (GBR 12909): Role of N-aromatic, N-heteroaromatic, and 3-oxygenated N-phenylpropyl substituents on affinity for the dopamine and serotonin transporter
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A series of N-aromatic, N-heteroaromatic, and oxygenated N-phenylpropyl derivatives of 1-(2-benzhydryloxyethyl)-piperazine and 1-{2-[bis-(4-fluorophenyl)methoxy]ethyl}piperazine, analogues of GBR 12909 (1a) and 12935 (1b), was synthesized and examined for their dopamine (DAT) and serotonin (SERT) transporter binding properties. One of these compounds, racemic 3-[4-(2-benzhydryloxyethyl)piperazin-1-yl]-1-(3-fluorophenyl)-propan-1-ol (33), had DAT affinity as good as, or better than, GBR 12909 and 12935, and was more selective for DAT over SERT than the GBR compounds. Both trans- (43) and cis- (47) (±)-2-(4-{2-[bis-(4-fluorophenyl)-methoxy]ethyl}piperazin-1- ylmethyl)-6-methoxy-1,2,3,4-tetrahydronaphthalen-1-ol had relatively good SERT selectivity and, as well, showed high affinity for SERT.
- Lewis, David,Zhang, Ying,Prisinzano, Thomas,Dersch, Christina M.,Rothman, Richard B.,Jacobson, Arthur E.,Rice, Kenner C.
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p. 1385 - 1389
(2007/10/03)
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- Substituted amino compounds and their use as substances having an analgesic effect
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Substituted amino compounds of general formula (I) are described, as are a method of preparing them and their use as drugs, especially as analgesics.
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- A synthetic approach to benanomicin A. 1. Synthesis of 5,6-dihydrobenzo[a] naphthacenequinone
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5,6-Dihydrobenzo[a] naphthacenequinone has been constructed by DIELS-ALDER reaction of an outer-ring diene with a naphthoquinone regioselectively. Similarly, the 14-hydroxy-5,6-dihydrobenzo[a] naphthacenequinone has also been synthesized via the reaction of vinylketene acetal with naphthoquinone.
- Hirosawa, Sehei,Nishizuka, Toshio,Kondo, Shinichi,Ikeda, Daishiro,Takeuchi, Tomio
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p. 685 - 689
(2007/10/03)
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- A modified Mannich reaction using 1,3-dioxolane
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Mannich reaction of ketones using 1,3-dioxolane instead of formaldehyde, paraformaldehyde, or 1,3,5-trioxane afforded the corresponding Mannich bases in high yields. Under the same conditions the aminomethylation of aromatics did not proceed but the intramolecular aminomethylation, like a Pictet-Spengler type reaction, proceeded smoothly.
- Sumita,Koumori,Ohno
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p. 1676 - 1678
(2007/10/02)
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- Intramolecular photocyclizations of amino ketones to form fused and bridged bicyclic amines
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The irradiation of cyclic aminoketones produces bicyclic amines derived from intramolecular electron transfer followed by cyclization.
- Kraus, George A.,Chen, Li
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p. 7151 - 7154
(2007/10/02)
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- α-Aminoalkylation of Enamines with Iminiumtetrachloro-aluminates
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We report the use of iminiumtetrachloro-aluminates 1a, 2a, and 3a in Mannich reactions.These salts are easily synthesized and offer some important advantages compared to iminium salts 1b-e. - Keywords: Iminiumtetrachloro-aluminates, Preformed Mannich Salts, α-Aminoalkylation, Enamines
- Risch, Nikolaus,Esser, Achim
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p. 208 - 210
(2007/10/02)
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- Nitrones and Oxaziridines. XXXI. Synthesis of Some Bicyclic 1-Pyrroline 1-Oxides
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The bicyclic 1-pyrroline 1-oxides (10), (11) and (13) have been prepared by reductive cyclization of the respective γ-nitro ketones (3), (4) and (6).Reduction of nitro ketone (2a) gave the unstable nitrone (7), which underwent dimerization to compound (8)
- Black, David St. C.,Johnstone, Lynn M.
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p. 117 - 128
(2007/10/02)
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- Analgesic and tranquilizing activity of 5,8 disubstituted 1 tetralone Mannich bases
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5,8-Disubstituted 1-tetralone Mannich bases represent semirigid variants of classical (i.e., chlorpromazine) neuroleptic agents. 8-Chloro-5-methoxy-2- morpholinomethyl-1-tetralone exhibits neuroleptic potency in the thiothixene range in animal models. Of greater potential interest, however, is the analgesic potency of the 8-chloro-5-methoxy-2-pyrrolidinomethyl analogue which was in the morphine range. This compound did not induce tolerance nor was its activity reversed by naloxone. Structure-activity relationships of the series are discussed.
- Welch,Harbert,Sarges,Stratten,Weissman
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p. 699 - 705
(2007/10/04)
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