- Highly atom economical uncatalysed and I2-catalysed silylation of phenols, alcohols and carbohydrates, using HMDS under solvent-free reaction conditions (SFRC)
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An uncatalysed silylation of phenols, regardless on the aggregate state and nature of the substituents with 0.55 equiv of HMDS under solvent-free reaction conditions (SFRC) at room temperature is reported. Sterically hindered phenols, carbohydrates and most of the alcohols additionally required a catalytic amount (up to 2 mol %) of iodine. The reaction protocol is very simple; obtaining a pure product, particularly of uncatalysed reactions, was frequently a completely solvent-free process.
- Jereb, Marjan
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experimental part
p. 3861 - 3867
(2012/06/30)
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- Effects of Structural Factors in Silyl Ethers Derived from Terminal Acetylenic Alcohols on 1,4-O→Csp Migration of the Silyl Group
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Effects of structural factors in silyl ethers derived from terminal acetylenic alcohols on 1,4-O-→Csp migration of the silyl group in the Iotsitch reagent were studied. The effect of steric factor at the carbon atom neighboring to the reaction center was found to be stronger than that at the silicon atom in the migrating group.
- Medvedeva,Novokshonov,Mareev,Borisova
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p. 336 - 339
(2007/10/03)
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- Synthesis and anti-aggregative activity of novel ω-achiral carba-analogues of prostacyclin
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Novel stable bicyclo[3.3.0]octanic and bicyclo[4.2.0]octanic 13,14-didehydrocarbacyclins 1a-c, 2a bearing an achiral cyclohexanoic group at C-14 were synthesized. These analogues have been characterized by 13C NMR spectroscopy. Compounds 1a-c and 2a were tested on rabbit and human platelet-rich blood plasma and 1a-c on rat stomach and guinea pig trachea smooth muscles. E-isomers of 1a-b were found to be less active but more selective than PGE1. The anti-aggregative potency of E-isomer of compounds 1a-b and Z-isomer of 2a on human platelets was 10-1-10-2 of the activity of PGE1. The contractive activity of bicyclo[3.3.0]octane analogues 1a-c was 10-3-10-4 of that for PGE1. On platelets and guinea-pig trachea 5E-isomers of the corresponding analogues were more potent, whereas on rat stomach muscle 5Z-isomers were.
- Lopp,Kobzar,Bergmann,Pehk,Lopp,Valimae,Viigimaa,Lille
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p. 155 - 159
(2007/10/02)
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- AN EFFICIENT CONVERSION OF KETO GROUPS INTO DIHYDROXYACETONE GROUPS: OXIDATION OF ETHYNYLCARBINOL INTERMEDIATES BY USING HYPERVALENT IODINE REAGENT
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A short and efficient synthesis of dihydroxyacetone groups from keto groups involving the oxidation of ethynylcarbinol intermediates with benzene (PIFA), is described.
- Tamura, Yasumitsu,Yakura, Takayuki,Haruta, Jun-ichi,Kita, Yasuyuki
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p. 3837 - 3840
(2007/10/02)
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- 1-Hydroxymethyl-1-1-oxo prostane derivatives of the E and F series
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The invention disclosed herein relates to pharmacologically active prostaglandin derivatives of the E, F, or A series having on the terminal methylene carbon of the alpha chain a substituent selected from the group consisting of: STR1 wherein R is an alkyl group and R15 is C1 -C4 alkyl, C1 -C4 alkoxy, di-C1 -C4 -alkylamino, and phenyl orphenyl substituted with one or more substituents selected from the group consisting of C1 -C4 alkyl, OR, SR, F, or Cl wherein R is as previously defined.
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- 1-Substituted-1-oxo-prostane-derivatives of the E, A and F series
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The invention disclosed herein relates to pharmacologically active prostaglandin derivatives of the E, F, or A series having on the terminal methylene carbon of the alpha chain, a substituent selected from the group consisting of: STR1 wherein R is C1 to C6 alkyl, and phenyl or phenyl substituted with one or more substituents selected from the group consisting of C1 -C4 alkyl, OR16, SR16, F, or Cl, and R16 is C1 to C6 alkyl.
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- Prostenoic acids and esters
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This disclosure describes derivatives, analogs, and congeners of prostanoic acid having a terminal cyclic moiety in the β-chain which possess the pharmacological activities associated with the prostaglandins.
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- Prostenoic acids and esters
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This disclosure describes derivatives, analogs, and congeners of prostanoic acid having a terminal cyclic moiety in the β-chain which possess the pharmacological activities associated with the prostaglandins.
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- Prostenoic acids and esters
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This disclosure describes derivatives, analogs, and congeners of prostanoic acid having a terminal cyclic moiety in the β-chain which possess the pharmacological activities associated with the prostaglandins.
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- 11-(2-Hydroxyethylthio) prostenoic acid E and F series derivatives
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This disclosure describes certain 11-(2-hydroxyethylthio) prostenoic acid E and F series derivatives, and their intermediates, useful as bronchodilators and inflammatory medeator release inhibitors.
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- An efficient method for the trimethylsilylation of tertiary alcohols
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Tertiary acetylenic alcohols have been transformed into the O-trimethylsilyl derivatives with trimethylsilyl chloride and triethylamine, using catalytic amounts of dimethyl sulfoxide, hexamethylphosphoric triamide, imidazole, or 1,5-diazabicyclound
- Visser, R. G.,Bos, H. J. T.,Brandsma, L.
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- 1-Hydroxymethyl-1-oxo-prostane derivatives of the E2 series
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Derivatives, analogs, and congeners of prostane having a 1-(hydroxymethyl)-1-oxo-prostane structure in the E2 series.
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- Prostenoic acids and esters
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This disclosure describes derivatives, analogs, and congeners of prostanoic acid having a terminal cyclic moiety in the β-chain which possess the pharmacological activities associated with the prostaglandins.
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- 11-(2-Hydroxyethylthio)prostenoic acid E2 series derivatives
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This disclosure describes certain 11-(2-hydroxyethylthio)-9-keto-prostenoic acid E series derivatives, and their intermediates, useful as bronchodilators and inflammatory medeator release inhibitors.
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