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Stereoselective synthesis of zooxanthellactone

The marine polyunsaturated natural product zooxanthellactone was synthesized in six steps and in 11% overall yield from eicosapentaenoic acid. The key synthetic steps were a Sonogashira cross-coupling reaction and a stereoselective semi-reduction. These efforts, together with NMR and optical rotation data, confirmed the reported structure of zooxanthellactone.

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Synthesis of New Optically Active Bis- and Tris(phosphines)

The synthesis of new optically active alkanediylbis- and alkanetriyltris(diphenylphosphines) is described.Easily accessible optically pure lactones and carboxylic acids are reduced to the alcohols, tosylated and reacted with lithium diphenylphosphide to give the corresponding phosphines.

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Aminoquinazolines and their use as medicaments

Compounds of the formula 1having an inhibitory effect on signal transduction mediated by tyrosine kinases, their use in the treatment of diseases, especially tumoral diseases and diseases of the lungs and air-ways, and the preparation thereof

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HETEROCYCLIC COMPOUND

The present invention provides a heterocyclic compound having an RORgammat inhibitory action. The present invention relates to a compound represented by the formula (I): wherein Ar is a the partial structure (1) to the partial structure (5), Q is a bivalent group selected from the group consisting of (Ia)-(If), and B is a ring optinally having substituent(s), or a salt thereof.

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Synthesis of Chiral Hydroxylated Quinolizidines via Vinylogous Bischler-Napieralski Nitrilium Ion Cyclizations

Treatment of the amido esters 9 and 17 with PPSE (polyphosphoric acid trimethylsilyl ester) followed by NaBH4 in ethanol gave the quinolizidinones 11-14 and 19 via a vinylogous Bischler-Napieralski nitrilium ion cyclization-reductive lactamization two-step process.Subsequent ozonolysis and reduction afforded chiral hydroxylated quinolizidines in moderate to good yield.In contrast to five-membered-ring formation, six-membered-ring formation via nitrilium-ion cyclization requires a p-methoxy-substituted styryl terminator.The effect para-substituted styryl terminators have on the energy of activation and DeltaH for the cyclization process has been calculated by semiempirical and ab initio methods.

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Organic acid salt of amlodipine

Disclosed are a novel organic acid salt of amlodipine with superb physicochemical properties, its preparation method, and a pharmaceutical composition containing the same as a therapeutically active ingredient.

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Radical cyclizations of acylsilanes in the synthesis of (+)-swainsonine and formal synthesis of (-)-epiquinamide

Radical cyclization of acylsilane is an useful synthetic methodology. To demonstrate the versatility of this method using the cyclization as a key step, polyhydroxylated indolizidine (+)-swainsonine was synthesized through two different bond connection approaches to construct the bicyclic skeleton. In the first approach, we used 2,3-isopropylidene-d-ribono-1,4-lactone (20) as a chiral building block to form the indolizidine skeleton through a 1,6-cyclization. In the second approach, (S)-(+)-5-oxo-2-tetrahydrofurancarboxylic acid (23) was used to construct the same ring system through a 1,5-cyclization. Starting from acid 23, we also synthesized exo-1-hydroxyquinolizidin-4-one (56), which was a synthetic intermediate in the synthesis of polyhydroxylated quinolizidine (-)-epiquinamide. 2011 Elsevier Ltd. All rights reserved.

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In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Application In Synthesis of (S)-( )-5-Oxo-2-tetrahydrofurancarboxylic Acid, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 21461-84-7, name is (S)-( )-5-Oxo-2-tetrahydrofurancarboxylic Acid. In an article£¬Which mentioned a new discovery about 21461-84-7

Stereospecific synthesis of (+)-muricatacin: A biologically active acetogenin derivative

(+)-muricatacin and analogs have been synthesized without ambiguity about the absolute configuration at the C-4 and C-5 centres. The observed [alpha](D) are reported as well as the results obtained for the cytotoxicity assay with KB and VERO cell lines.

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Asymmetric syntheses of 6-deoxyfagomin, d-deoxyrhamnojirimycin, and d-rhamnono-1,5-lactam

N-Allyl protected 3-O-benzyloxglutarimide 11 was synthesized as a useful variant of the chiral building block 10. This modification allowed a high-yielding deprotection of the allyl group from the lactam intermediate 14. Starting from this building block, the asymmetric syntheses of aza-sugars 6-deoxyfagomine (2), d-rhamnono-1,5-lactam (6), as well as d-deoxyrhamnojirimycin (5) have been achieved in high regio- and/or diastereo-controlled manner.

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Allyl Isopropenyl Dicarbonate; A Convenient Reagent for the Preparation of Allyl Esters of Carboxylic Acids

Allyl isopropenyl dicarbonate(1) reacts with carboxylic acids in the presence of 4-dimethylaminopyridine(DMAP) catalyst to give allyl esters in high yields under mild conditions such as in a near-neutral medium at room temperature.

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