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Recent advances in the chemistry of macroline, sarpagine and ajmaline-related indole alkaloids

The chemistry of indole alkaloids related to macroline, sarpagine, and ajmaline was investigated. The Pictet-Spengler reaction remains a key strategic transformation for the synthesis of molecules of indole alkaloids. The chemistry shows that considerable advances have been made in the field of indole alkaloids. Several macroline-related alkaloids have been isolated and it is believed that macroline,or an equivalent is a likely biosynthetic precursor of various sarpagine alkaloids. Ajmaline-related alkaloids are defined as those having the same skeletal connectivity as ajmaline with an N4-C21 linkage but with the C16-(S) configuration. Sarpagine-related alkaloids are defined as those having the same skeletal connectivity as sarpagine with N4-C21 linkage. It is expected that further advances in the chemistry of macroline/ sarpagine/ ajmaline indole alkaloids will be reported by many laboratories.

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Reference£º
Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI

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Final-stage site-selective acylation for the total synthesis of natural glycosides

The first total syntheses of multifidosides A-C are reported. The prominent feature is an unconventional retrosynthesis based on organocatalytic site-selective acylation of unprotected glycosides at the final stage of synthesis. A notable advantage of this strategy is that it avoids the risks of undesired side reactions during the removal of the protecting groups at the final stage of total synthesis. The proposed synthetic strategy has another advantage in terms of efficient late-stage derivatization of natural products. Due to the predictability and reliability of the catalytic site-selective introduction of various functionalized acyl groups, the present synthetic strategy could provide a general synthetic route to 4-O-acylglycosides, such as phenylethanoid glycosides and ellagitannins, which are of biological interest.

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Reference£º
Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI

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Metal-Free and Selective Oxidation of Benzylic Alcohols to Aromatic Aldehydes by Hexachloroacetone

A metal-free and selective oxidation of benzylic alcohols which leads to the direct and sustainable production of benzaldehydes has been developed. Compared with former known oxidation reactions like Swern, Pfitzner-Moffatt, Parikh-Doering, and Corey-Kim oxidations, this oxidation approach introduces the HCA as an easily available, safer and less expensive reagent, and also because of the simple removing of chloroform. In addition, it is not necessary to add any metal, acid or base for the oxidation of benzylic alcohols. The oxidation is proceeded in DMSO and also under solvent-free conditions in excellent yields.

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Reference£º
Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI

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Synthesis of the Cyanobacterial Antibiotics Anaephenes A and B

The first syntheses of the antibacterial natural products anaephenes A (1) and B (2) are reported. Both natural products were synthesized in five linear steps from commercially available tert-butyl(3-iodophenoxy)dimethylsilane. Key steps for the synthesis included a Sonogashira cross-coupling and a Julia-Kocienski olefination to selectively construct the E-alkene present in the natural products. This synthetic route allowed the identities and antimicrobial activities of anaephenes A (1) and B (2) to be confirmed. Additionally, these compounds displayed antimicrobial activity against methicillin-resistant Staphylococcus aureus (MRSA) with MIC values of 16 and 8 mug/mL, respectively.

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Reference£º
Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI

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Pyrazole containing benzofuran derivatives and pharmaceutical compositions

The invention provides compounds of formula (I): STR1 or a physiologically acceptable salt, solvate or metabolically labile ester thereof. The compounds may be used in the treatment or prophylaxis of hypertension and diseases associated with cognitive disorders.

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Reference£º
Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI

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A highly enantioselective total synthesis of (+)-goniodiol

A high-yielding enantioselective total synthesis of the bioactive styryllactone (+)-goniodiol has been realised, starting from readily available (S)-glycidol. A key step is an oxygen-to-carbon rearrangement of a silyl enol ether linked via an anomeric centre, facilitating the rapid and diastereoselective construction of this functionalised system. The Royal Society of Chemistry 2006.

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Reference£º
Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI

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14-deoxy-14alpha-cardenolides 3beta-thioderivatives and pharmaceutical composition comprising same for treating cardiovascular disorders

14-Deoxy-14alpha-cardenolides 3beta-thioderivatives and pharmaceutical compositions comprising same for treating cardiovascular disorders, such as heart failure and hypertension, are disclosed.

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Reference£º
Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI

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Tetra-N-propylammonium perruthenate: A case study in catalyst recovery and re-use involving tetraalkylammonium salts

The use of tetraalkylammonium salts or imidazolium ionic liquids in catalytic oxidations of alcohols with tetra-N-propylammonium perruthenate allows recovery and reuse of the oxidant; this concept may find application in the recovery of other homogenous catalysts.

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Reference£º
Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI

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CCR3 antagonists: A potential new therapy for the treatment of asthma. Discovery and structure-activity relationships

CCR3 antagonist leads with IC50 values in the muM range were converted into low nM binding compounds that displayed in vitro inhibition of human eosinophil chemotaxis induced by human eotaxin. In particular, 4-benzylpiperidin-1-yl-n-propylureas and erythro-3-(4-benzyl-2-(alpha-hydroxyalkyl)piperidin-1-yl)-n-propylureas (obtained via Beak reaction of N-BOC-4-benzylpiperidine) exhibited single digit nanomolar IC50 values for CCR3.

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Reference£º
Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI

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Electron Spin Resonance Spectra of the Perruthenate(VII) Ion, (1-)

Electron spin resonance spectra of the (1-) ion , where A = NPrn4, N(PPh3)2 or PPh4> in frozen glasses of dichloromethane at ca. 90 K have been recorded; for A = NPrn4, gx = 1.93, gy = 1.98 and gz = 2.06.The spectrum of (1-) (and its electronic spectrum) have been interpreted and compared with those of an alkaline aqueous solution containing ruthenium(VII) species.The ESR spectrum of powdered potassium ruthenate(VI), trans-K2, at ca. 90 K was also recorded, and the preparation of , a new salt of (1-), is described.

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Reference£º
Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI