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Tetrahydrofuran antifungals

A compound represented by the formula I STR1 wherein X is independently both F or both Cl or one X is independently F and the other is independently Cl; R1 is a straight or branched chain (C3 to C8) alkyl group substituted by one or two phosphate ester groups (e.g., a phosphate ester convertible in vivo into a hydroxy group) thereof or a pharmaceutically acceptable salt thereof and pharmaceutical compositions thereof useful for treating and/or preventing fungal infections are disclosed.

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Reference:
Synthesis and Crystal Structure of a Chiral C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur–nitrogen–oxygen ligand derived from aminothiourea and sodium D-camphor-β-sulfonate

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Production of (2S,3S)-2,3-butanediol and (3S)-acetoin from glucose using resting cells of Klebsiella pneumonia and Bacillus subtilis

Production of highly pure (2S,3S)-2,3-butanediol ((2S,3S)-2,3-BD) and (3S)-acetoin ((3S)-AC) in high concentrations is desirable but difficult to achieve. In the present study, glucose was first transformed to a mixture of (2S,3S)-2,3-BD and meso-2,3-BD by resting cells of Klebsiella pneumoniae CICC 10011, followed by biocatalytic resolution of the mixture by resting cells of Bacillus subtilis 168. meso-2,3-BD was transformed to (3S)-AC, leaving (2S,3S)-2,3-BD in the reaction medium. Using this approach, 12.5gl-1 (2S,3S)-2,3-BD and 56.7gl-1 (3S)-AC were produced. Stereoisomeric purity of (2S,3S)-2,3-BD and enantiomeric excess of (3S)-AC was 96.9 and 96.2%, respectively.

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Reference:
Synthesis and Crystal Structure of a Chiral C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur–nitrogen–oxygen ligand derived from aminothiourea and sodium D-camphor-β-sulfonate

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Kinetic Resolution of Oxiranes by Chiral Molybdenum(VI) (Oxodiperoxo) alpha-Hydroxy Acid Amide/Diol Reagents

In situ formed chiral molybdenum(VI) (oxodiperoxo) hydroxy acid amide/aliphatic diol complexes mediate the efficient kinetic resolution of simple unfunctionalized oxiranes in the presence of molecular oxygen. This method furnishes high enantiomeric yields at reasonable chemical yields for the residual chiral oxiranes.

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Reference:
Synthesis and Crystal Structure of a Chiral C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur–nitrogen–oxygen ligand derived from aminothiourea and sodium D-camphor-β-sulfonate

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CHIRAL SYNTHESIS OF (2S,3S,7S)-3,7-DIMETHYLPENTADECAN-2-YL ACETATE AND PROPIONATE, POTENTIAL SEX PHEROMONE COMPONENTS OF THE PINE SAW-FLY NEODIPRION SERTIFER (GEOFF.)

A synthesis of (2S,3S,7S)-3,7-dimethylpentadecan-2-yl acetate (2) and propionate (3) is described. (2S)-2-Methyldecan-1-yl lithium (5) was reacted with (3S,4S)-3,4-dimethyl-gamma-butyrolactone (6) to yield the ketoalcohol 19 which upon Huang-Minlon reduction furnished (2S,3S,7S)-3,7-dimethylpentadecan-2-ol (1).Acylations gave the esters 2 and 3.The (2S)-2-methyldecan-1-yl lithium was obtained via asymmetric synthesis.The chiral lactone 6 was obtained from (2S,3S)-trans-2,3-epoxybutane and dimethylmalonate.

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Reference:
Synthesis and Crystal Structure of a Chiral C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur–nitrogen–oxygen ligand derived from aminothiourea and sodium D-camphor-β-sulfonate

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MACROCYCLIC GHRELIN RECEPTOR MODULATORS AND METHODS OF USING THE SAME

The present invention provides novel conformationally-defined macrocyclic compounds that can function as selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, bone disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.

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Reference:
Synthesis and Crystal Structure of a Chiral C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur–nitrogen–oxygen ligand derived from aminothiourea and sodium D-camphor-β-sulfonate

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Synthesis of New Optically Active Crown Ethers

Optically active crown ethers 1a-11, 2, 3a,b, 4a,b, 5a,b and the analogue 6 are synthesized.The efficiency of these compounds as phase-transfer catalysts for a series of enantioselective reactions will be tested.This will be described in a following publication. Key Words: Crown ethers, chiral, optically active / Phase transfer catalysts

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Reference:
Synthesis and Crystal Structure of a Chiral C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur–nitrogen–oxygen ligand derived from aminothiourea and sodium D-camphor-β-sulfonate

Brief introduction of C4H10O2

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Properties of diacetyl (acetoin) reductase from Bacillus stearothermophilus

The cells of Bacillus stearothermophilus contain an NADH-dependent diacetyl (acetoin) reductase. The enzyme was easily purified to homogeneity, partially characterised, and found to be composed of two subunits with the same molecular weight. In the presence of NADH, it catalyses the stereospecific reduction of diacetyl first to (3S)-acetoin and then to (2S,3S)-butanediol; in the presence of NAD+, it catalyses the oxidation of (2S,3S)- and meso-butanediol, respectively to (3S)-acetoin and to (3R)-acetoin, but is unable to oxidise these compounds to diacetyl. The enzyme is also able to catalyse redox reactions involving some endo-bicyclic octen- and heptenols and the related ketones, and its use is suggested also for the recycling of NAD+ and NADH in enzymatic redox reactions useful in organic syntheses.

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Reference:
Synthesis and Crystal Structure of a Chiral C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur–nitrogen–oxygen ligand derived from aminothiourea and sodium D-camphor-β-sulfonate

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SYNTHESE DIASTEREOSELECTIVE D’UNE COMPOSANTE DE LA PHEROMONE SEXSUELLE DE “L’ECAILLE ROUGE DE CALIFORNIE” : L’ACETATE D’ISOPROPENYL-6 METHYL-3 DECENE-9 YLE(3S, 6R)

6-Isopropenyl 3-methyl 9-decene yl acetate (3S, 6R) has been synthesized from readily available trans(-)-dihydrocarvone.Regioselective ozonolysis of this ketone silyl enol ether is the key step of the sequence and allows to preserve both chiral centers.

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Reference:
Synthesis and Crystal Structure of a Chiral C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur–nitrogen–oxygen ligand derived from aminothiourea and sodium D-camphor-β-sulfonate

Properties and Exciting Facts About (2S,3S)-Butane-2,3-diol

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Compounds and Their Use in Treating Cancer

The specification generally relates to compounds of Formula (I): and pharmaceutically acceptable salts and prodrugs thereof, where R1, R4, R5, R6, R7, Linker, X, Y, A, G, D and E have any of the meanings defined herein. This specification also relates to the use of such compounds and pharmaceutically acceptable salts and prodrugs thereof in methods of treatment of the human or animal body, for example in prevention or treatment of cancer. This specification also relates to processes and intermediate compounds involved in the preparation of such compounds and to pharmaceutical compositions containing them.

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Reference:
Synthesis and Crystal Structure of a Chiral C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur–nitrogen–oxygen ligand derived from aminothiourea and sodium D-camphor-β-sulfonate

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Stereospecific conversion of chiral 1,2-cyclic sulfates to chiral imidazolines

The one pot preparation of imidazolines from 1,2-cyclic sulfates is reported. Amidines react with cyclic sulfates to give zwitterionic intermediates, and subsequent intramolecular cyclization affords imidazolines. The preparation of enantiopure stilbene diamine (stien) is achieved by the hydrolysis of its corresponding chiral imidazoline.

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Reference:
Synthesis and Crystal Structure of a Chiral C3-Symmetric Oxygen Tripodal Ligand and Its Applications to Asymmetric Catalysis,
Chiral lanthanide(III) complexes of sulphur–nitrogen–oxygen ligand derived from aminothiourea and sodium D-camphor-β-sulfonate