- PROCESS FOR SYNTHESIS OF ANDROSTANE 17-BETA CARBOTHIOIC ACID AND RELATIVE COMPOUNDS THEREOF
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A process for synthesis of androstane 17-β carbothioic acid is provided. The process includes mixing an androstane 17-β carboxylic acid and a coupling reagent, and adding an alkanethioic acid to form an androstane 17-β carbothioic acid, wherein the androstane 17-β carbothioic acid has the formula (I): wherein R1 represents hydrogen or haloalkyl groups, R2 represents C1-8 linear alkyl groups, C1-8 branched alkyl groups, C1-6 unsaturated acyclic groups or aromatic groups, R3 represents hydrogen or hydroxyl, R4 represents hydrogen, bromine, chlorine or fluorine and R5 represents hydrogen, bromine, chlorine or fluorine. The process is a one-pot reaction.
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(2009/12/02)
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- High percentage beta-yield synthesis of carbapenem intermediates
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Disclosed herein is a novel process using novel silyl enol ether intermediates of the formula STR1 to generate novel azetidione thiolester intermediates of the formula STR2 which can be used to form 1-β-alkyl carbapenem antibiotics. It has now been discovered that if the R4 group is selected from a small group of moieties having the formula: STR3 an increased β-yield of up to approximately 100% can be obtained.
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- 4-Androsten-3-ones and process for the preparation thereof
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4-Androsten-3-ones of the formula STR1 wherein R1 is hydrogen or the acyl radical of an organic or inorganic acid, R2 is hydrogen, alkyl, or the acyl radical of an organic or inorganic acid, R3 is methyl or ethyl, R4 is hydrogen or methyl, STR2 and R5 is lower alkyl, have diuretic activity.
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- Pesticidal compositions containing phosphoric esters and divalent sulphur compounds
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Pesticidal composition comprising: a pesticidal, phosphoric ester the molecule of which has at least one alkyl group of 1 to 3 carbon atoms, 0.05 to 10% of an agent stabilizing the said ester against decomposition by protonisation, together with adjuvants characterized in that the stabilizing agent comprises at least one sulphur compound containing per molecule at least one divalent sulphur atom of which one valence is bonded to an atom chosen from sulphur, carbon, nitrogen, hydrogen, and metals capable of giving a salt, the other valence being bonded to an atom chosen from hydrogen, the carbon atom already noted, a second carbon atom, the nitrogen atom already noted, a second nitrogen atom, the metal atom already noted in the case of a metal of valence greater than one, a second atom of metal and oxygen when the first valence is not attached to an atom of hydrogen, the proportion of sulphur calculated with reference to the weight of the sulphur compound being between 5 and 99%. Process for stabilizing a phosphoric ester of which the molecule possesses at least one alkyl group containing 1 to 3 carbon atoms characterized in that there is added to the phosphoric ester or to a mixture which contains it, 0.05 to 10% calculated on the weight of the phosphoric acid ester of an agent capable of stabilizing the said phosphoric ester against protonisation and comprising at least one sulphur compound such as that defined thereupon.
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