Abstract: The present invention relates to a process for the preparation of 4-aminomethyl-3-alkoxyiminopyrrolidine methane-sulfonate, a key intermediate of quinolone antibiotics. According to the process of the present invention, the total number of steps has been shortened to 2-3 steps, the solid separation is not required, and the use of costly chemicals, particularly (BOC)2O (t-butoxycarbonyl anhydride), several organic solvents and reactants, is eliminated.

Abstract: Starting from ethyl 3-(2,6-dichloro-5-fluoropyridin-3-yl)-3-oxo-propanoate (1), the present invention provides highly pure 7-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid (5) inone-potfour stepsusing a single solvent.

Abstract: The present invention relates to a process for preparing 4-chloro-3-hydroxybutanoic acid ester, an intermediate for preparing atorvastatin, in high purity and yield, by comprising the steps of 1) reacting epichlorohydrin of formula (2) with cyanide of formula (3) under the condition of pH ranging from 7 to 8, to form the 4-chloro-3-hydroxybutyronitrile of formula (4) and 2a) dissolving the 4-chloro-3-hydroxybutyronitrile of formula (4) in an alcoholic solvent and reacting it with hydrogen chloride, or 2b) reacting the 4-chloro-3-hydroxybutyronitrile of formula (4) in an alcoholic solvent saturated with hydrogen chloride, to form the 4-chloro-3-hydroxybutyronitrile acid ester of formula (I).

Abstract: The present invention relates to an isoxazoline derivative as an inhibitor against various caspases, a process for preparing the same, and a therapeutic composition for preventing inflammation and apoptosis comprising the same

Abstract: The present invention relates to a process for the preparation of 4-aminomethyl-3-alkoxyiminopyrrolidine methane-sulfonate, a key intermediate of quinolone antibiotics. According to the process of the present invention, the total number of steps has been shortened to 2-3 steps, the solid separation is not required, and the use of costly chemicals, particularly (BOC)2O (t-butoxycarbonyl anhydride), several organic solvents and reactants, is eliminated.

Abstract: The present invention is related to a novel process for preparing an optically active 5-hydroxy-3-oxo-hexanoic acid derivative or its tautomer which is useful intermediate for preparing statins such as atorvastatin and rosuvastatin. Blaise reaction of (S)-4-halo-3-hydroxybutyronitrile with -haloacetate is utilized as a key reaction to provide the product with minimal formation of side products and in good yield.

Abstract: The present invention is related to a novel process for preparing an optically active 5-hydroxy-3-oxo-hexanoic acid derivative or its tautomer which is useful intermediate for preparing statins such as atorvastatin and rosuvastatin. Blaise reaction of (S)-4-halo-3-hydroxybutyronitrile with -haloacetate is utilized as a key reaction to provide the product with minimal formation of side products and in good yield.

Abstract: The present invention relates to a new process for preparing beta-ketoester compound of the following formula (1), which is a useful intermediate for the synthesis of such quinoline antibiotics as Ciprofloxacin, Levofloxacin, Gemifloxacin, Trovafloxacin, etc. The quinoline antibiotics obtained from the above compound of formula (1) show potent antibacterial activity, and so are advantageously used as a therapeutic agent for bacterial infections of humans or animals.

Abstract: A wideband 180° bit phase shifter has a simplified circuit construction by using a grounded switching device. The wideband 180° bit phase shifter includes a Lange coupler having an input port, an output port, a through port and a coupled port; and reflective loads respectively connected to the through port and the coupled port of the Lange coupler in order to reflect inputted radio signals.

Abstract: A process for preparing a 1-substituted 5-hydroxymethylimidazole of the formula: , wherein R represents alkyl, hydroxyalkyl, allyl, or substituted or unsubstituted arylmethyl or diarylmethyl, comprising the step of reacting a 1-substituted 2-mercapto-5-hydroxymethylimidazole of the formula: , wherein R is as defined above, in the presence of a transition metal catalyst and an oxidizing agent in a solvent.

Abstract: The present invention relates to a novel process for preparing pyrrole ester compounds, which are key intermediates in the preparation of farnesyl transferase inhibitors, an anti-cancer agent Horner-Emmons reaction of aldehyde compounds provides the corresponding &agr;,&bgr;-unsaturated esters, which without any separation and/or purification steps, are treated with toluenesutfonyl-methylisocyanate in the presence of base to give pyrrole esters in one-pot fashion.

Abstract: The present invention relates to a novel process for preparing pyrrole ester compounds, which are key intermediates in the preparation of farnesyl transferase inhibitors, an anti-cancer agent. Horner-Emmons reaction of aldehyde compounds provides the corresponding &agr;,&bgr;-unsaturated esters, which without any separation and/or purification steps, are treated with toluenesulfonylmethylisocyanate in the presence of base to give pyrrole esters in one-pot fashion.

Abstract: The present invention relates to a process for preparing a useful medicinal intermediate represented by the following formula (1): in which, R1, A and n are defined as described in the specification, or its stereoisomer, characterized in that a compound represented by the following formula (2): in which, R, R1, A and n are defined as described in the specification, is reacted with a cyanide in the presence of a nickel catalyst.