Takeda Chemical Industries, Inc.

Tohru Sugawara

Nobuyoshi Hayashi

Yasuhiko Kawano

Hirotomo Masuya

Taisuke Matsuo

Kouichi Yoshioka

Takuichi Miki

Shinji Kato

An automatic synthesizing apparatus for continuously effecting automatically by a controlling apparatus all the operations including the supplying of samples into reaction vessel and so on, reaction processing of the contents within the reaction vessels, PH adjustment, extraction/dehydration processing, purification of the contents, and further analysis of the reaction condition so as to produce the target compounds. Many basic unit operation procedures are made and stored so that programs for effecting the operation controlling of the automatic synthesizing apparatus may be extremely easily made. The innumerable syntheses programs in the chemical experiments may be effected simply by the inputting of the operation names of the unit operation procedures in the operational orders when the synthesis order programs may be made for each target compound.

Automated synthesis apparatus and method of controlling the apparatus

an automated synthesizing apparatus which comprises a raw material, reagent and solvent supply unit, a reaction unit, a purification unit provided with HPLC and CPC, and a freeze-drying unit for freeze-drying a purified product supplied from the purification unit. The raw material, reagent and solvent supply unit includes a plurality of reservoirs for containing raw material, reagents and solvents; volumetric tubes and gas-liquid boundary sensors for the quantification of the raw material, reagents and solvents from the reservoirs; flow-lines for supplying the raw material, reagent and solvent from the reservoirs towards subsequent steps; and solenoid valve assemblies disposed on the respective flow-lines for selectively closing and opening such respective flow-lines. The reaction unit includes a reaction flask device adapted to receive the raw material from the raw material, reagent and solvent supply unit; a separation funnel for extracting or washing a product which is transferred from the reaction flask device; a pH adjusting flask for adjusting acidity or basicity of the reaction liquid from the separation funnel; a plurality of reagent reservoirs disposed for adding a predetermined quantity of reagent to the reaction flask device, volumetric tubes and gas-liquid boundary sensors. All of the units, the sensors and the solenoid valve assemblies of each of the units are so connected with a computer that the sequence of operation thereof can be controlled thereby.

Automated synthesizing apparatus

A computerized compound synthesization for producing an aimed product by controlling a synthesis reaction process including steps of supplying raw material compounds, reagents and solvents, a synthesis reaction step, a purification step and a product extraction step in accordance with a control program. Optimal condition for the reaction is established by determining discrete time points at which the reagent is added and volumes of the reagent to be added at the time points, respectively, on the basis of parameters including reaction rate constant, equilibrium, constant, initial concentration of starting material mixture, ratio of concentration of intermediate product to theoretical equilibrium concentration, stoichiometrical ratio between the reagent and the intermediate and concentration of the reagent in accordance with a relation established among these parameters.

Automatic synthesis apparatus

An automated computer controlled synthesizing apparatus which includes a raw material, reagent and solvent supply unit, a reaction unit, a purification unit provided with HPLC and CPC, and a freeze-drying unit for freeze-drying a purified product supplied from the purification unit. The raw material, reagent and solvent supply unit includes a plurality of reservoirs for containing raw material, reagents and solvents; volumetric tubes and gas-liquid boundary sensors for the quantification of the raw materials, reagents and solvents from the reservoirs; flow-lines for supplying the raw material, reagent and solvent from the reservoirs towards subsequent steps; and solenoid valve assemblies disposed on the respective flow-lines for selectively closing and opening such respective flow-lines. The reaction unit includes a reaction flask device adapted to receive the raw material, reagent and solvent from the raw material, reagent and solvent supply units respectively, a separation funnel for extracting or washing a product which is transferred from the reaction flask device; a pH adjusting flask for adjusting acidity or basicity of the product liquid from the separation funnel; and a plurality of reagent reservoirs disposed for adding a predetermined quantity of reagent to the reaction flask device, volumetric tubes and gas-liquid boundary sensors.

Optically active .beta.-lactams of the general formula ##STR1## wherein R.sup.1 is an amino or protected amino group, R.sup.2 is an organic residue bonding through a carbon atom thereof and R.sup.3 is the residue remaining after removal of the .alpha.-amino group from an optically active .alpha.-amino acid or a derivative thereof as well as a method of producing the same.

Optically active .beta.-lactams and method of their production

Novel cephem compounds having a group of the formula at the 3-position thereof: ##STR1## wherein X represents oxygen, sulfur or imino, which may be substituted; and B represents hydrogen or a hydroxyl, amino, mercapto or hydrocarbon group, which groups may be substituted, can be prepared by reacting a 3-formylcephem compound with a hydrazine compound of the formula: ##STR2## wherein the symbols have the same meanings as above, and subjecting the thus obtained compound to an oxidative ring-closure reaction. The objective compounds are found to have a broad antimicrobial spectrum and, in particular, are effective against gram-negative bacteria including Escherichia Coli, Klebsiella pneumoniae, Proteus vulgaris, Proteus mirabilis, Proteus rettgerii, as well as gram positive ones, and have low-toxity. Thus, these compounds may be used for antimicrobial agents in therapeutical purpose.

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Osaka, Japan

Tohru Sugawara