Abstract: A process comprising reacting an aliphatic carboxylic ester compound with acetonitrile in the presence of a metal alkoxide to yield a metal salt of a ?-ketonitrile compound, subsequently transferring the salt to an aqueous medium, and neutralizing the solution to obtain the ?-ketonitrile compound in a free state, wherein a water-immisible organic solvent and water are added to the reaction mixture containing the ?-ketonitrile compound metal salt yielded to transfer the metal salt to the water, the resultant aqueous solution of the ?-ketonitrile compound metal salt is separated from the organic solvent by phase separation or another technique and then neutralized, and the resultant free ?-ketonitrile compound is taken out by extraction with an organic solvent.

Abstract: A process for preparing a dibenzothiazepine derivative such as dibenzo[b,f] [1,4]thiazepin-11-one employable as a starting material for the preparation of 11-[4-(2-(2-hydroxyethoxy)ethyl)]-1-piperadinyldibenzothiazepine derivative which is known to be effective as an antipsychotic pharmaceutical, has the steps of reacting a nitrobenzene derivative with a thiosalicylic acid derivative, reducing the obtained 2-nitro-2?-carboxy-diphenylsulfide derivative, and subjecting the obtained 2-amino-2?-carboxy-diphenylsulfide derivative to dehydration-condensation reaction.

Abstract: A 5-fluorooxindole-3-carboxylic acid ester represented by a formula (2): wherein R1 is a group selected from the group consisting of an unsubstituted or substituted alkyl group having 1 to 10 carbon atoms, an unsubstituted or substituted cycloalkyl group having 3 to 7 carbon atoms, an aralkyl group having 7 to 10 carbon atoms or an aryl group having 6 to 14 carbon atoms.

Abstract: A 4-aminoquinazoline derivative can be obtained by the steps of reacting quinazolin-4-one or its derivative with a chlorinating agent in a first organic solvent in the presence of an organic base, and subsequently reacting the reaction product with an amine compound represented by the formula R5—NH—R6 (each of R5 and R6 represents hydrogen or an optionally substituted hydrocarbyl group) in the presence of a second organic solvent.

Abstract: A process for preparing quinazolin-4-one or its derivative by reacting anthranilic acid or its derivative with formic acid or its derivative in the presence of ammonia, or by reacting ammonium anthranilate or its derivative with formic acid or its derivative.

Abstract: The present invention discloses a process for preparing 5-fluorooxindole represented by the formula (3): which comprises (A) a first step of cyclizing 2-(5-fluoro-2-nitrophenyl)malonic acid diester represented by the formula (1): wherein R1 and R2 may be the same or different from each other and each represents a group which does not participate in the reaction, under reductive conditions to form 5-fluorooxindole-3-carboxylic acid ester represented by the formula (2): wherein R1 has he same meaning as defined above, and (B) then, a second step of decarboxylating the 5-fluorooxindole-3-carboxylic acid ester, and a process for preparing its synthetic intermediates.

Abstract: A process for producing a quinazolin-4-one compound having the formula: [wherein R1, R2, R3 and R4 each represents a group not participating in the below-mentioned reaction, and R1, R2, R3 and R4 can be combined together to form a ring] which comprises reacting an anthranilic acid derivative having the formula: [wherein R5 is a hydrogen atom or a hydrocarbyl group] with a formic acid derivative in the presence of an ammonium carboxylate.

Abstract: 2-Cyclopropyl-4-(4?-fluorophenyl)quinoline-3-carboxyaldehyde useful as a material for pharmaceutical products, can be obtained by reacting 3-cyclopropyl-3-oxopropanenitrile with 2-amino-4?-fluorobenzophenone to obtain 2-cyclopropyl-4-(4?-fluorophenyl)quinoline-3-carbonitrile, and reducing it.

Abstract: 2-Cyclopropyl-4-(4′-fluorophenyl)quinoline-3-carboxyaldehyde useful as a material for pharmaceutical products, can be obtained by reacting 3-cyclopropyl-3-oxopropanenitrile with 2-amino-4′-fluorobenzophenone to obtain 2-cyclopropyl-4-(4′-fluorophenyl)quinoline-3-carbonitrile, and reducing it.

Abstract: A process comprising reacting an aliphatic carboxylic ester compound with acetonitrile in the presence of a metal alkoxide to yield a metal salt of a &bgr;-ketonitrile compound, subsequently transferring the salt to an aqueous medium, and neutralizing the solution to obtain the &bgr;-ketonitrile compound in a free state, wherein a water-immisible organic solvent and water are added to the reaction mixture containing the &bgr;-ketonitrile compound metal salt yielded to transfer the metal salt to the water, the resultant aqueous solution of the &bgr;-ketonitrile compound metal salt is separated from the organic solvent by phase separation or another technique and then neutralized, and the resultant free &bgr;-ketonitrile compound is taken out by extraction with an organic solvent.

Abstract: The present invention is to provide a process for producing a tetrahydropyranyl-4-sulfonate which comprises allowing 3-buten-1-ol which is easily available to react with a formaldehyde compound and an organic sulfonic acid, and a process for producing a 4-aminotetrahydropyrane derivative, which is industrially useful, under mild conditions and by a simple and easy method to produce the 4-aminotetrahydropyrane derivative in high yield.

Abstract: 3-[2-Cyclopropyl-4-(4-fluorophenyl)-3 quinolyl]prop-2-enal is prepared in a high yield by reducing 3-[2-cyclo-propyl-4-(4-fluorophenyl)-3-quinolyl]prop-2-enenitrile with Raney nickel either in the presence of formic acid and 0.25 to 1 part by volume of water per part by volume of formic acid or in the presence of both an amine salt of formic acid and an organic acid.

Abstract: The present invention discloses a process for preparing 5-fluorooxindole represented by the formula (3): 1

Abstract: 3-[2-Cyclopropyl-4-(4-fluorophenyl)-3-quinolyl]prop-2-enal is prepared in a high yield by reducing 3-[2-cyclopropyl-4-(4-fluorophenyl)-3-quinolyl]prop-2-enenitrite with Raney nickel either in the presence of formic acid and 0.25 to 1 part by volume of water per part by volume of formic acid or in the presence of both an amine salt of formic acid and an organic acid.

Abstract: 3-[2-Cyclopropyl-4-(4-fluorophenyl)-3-quinolyl]prop-2-enenitrile is prepared by reacting 2-cyclopropyl-4-(4-fluorophenyl)quinoline-3-carbaldehyde with acetonitrile in the presence of a base and then adding a dehydrating to the reaction mixture to conduct dehydration. Under ordinary conditions, novel 3-[2-cyclopropyl-4-(4-fluoro-phenyl)-quinolin-3-yl]-3-hydroxypropionitrile is formed as an intermediate in the above reaction. Incidentally, when the above reaction is conducted in an organic solvent, 3-[2-cyclopropyl-4-(4-fluorophenyl)-3-quinolyl]-prop-2-enenitrile is directly formed.

Abstract: 3-[2-Cyclopropyl-4-(4-fluorophenyl)-3-quinolyl]prop-2-enenitrite is prepared by reacting 2-cyclopropyl-4-(4-fluorophenyl)quinoline-3-carbaldehyde with acetonitrile in the presence of a base and then adding a dehydrating to the reaction mixture to conduct dehydration. Under ordinary conditions, novel 3-[2-cyclopropyl-4-(4-fluorophenyl)-quinolin-3-yl]-3-hydroxypropionitrile is formed as an intermediate in the above reaction. Incidentally, when the above reaction is conducted in an organic solvent, 3-[2-cyclopropyl-4-(4-fluorophenyl)-3-quinolyl]-prop-2-enenitrite is directly formed.

Abstract: The present invention is to provide a process for producing a tetrahydropyranyl-4-sulfonate which comprises allowing 3-buten-1-ol which is easily available to react with a formaldehyde compound and an organic sulfonic acid, and a process for producing a 4-aminotetrahydropyrane derivative, which is industrially useful, under mild conditions and by a simple and easy method to produce the 4-aminotetrahydropyrane derivative in high yield.

Abstract: A process for preparation of 2-(10,11-dihydro-10-oxodibenzo[b,f]thiepin-2-yl)propionic acid (i.e., Zaltoprofen) is performed by subjecting 2-(4-amino-3-carboxy-methylphenyl)propionic acid or its salt to diazotization and subsequent reaction with thiophenol to produce 2-(3-carboxymethyl-4-phenylthiophenyl)propionic acid or its salt, and subjecting the product to cyclization reaction. Other related processes and related compounds are also disclosed.

Abstract: Compounds of formula (I): ##STR1## wherein R.sup.1 is hydrogen, alkyl, halogen, haloalkyl, hydroxy, alkoxy, haloalkoxy, alkylthio, haloalkylthio, amino, alkanoyl, haloalkanoyl, carboxy, alkoxycarbonyl, carbamoyl, cyano, nitro, alkanesulfonyl, haloalkanesulfonyl or sulfamoyl; R.sup.2 is 5,6-dihydro-1,4,2-dioxazin-3-yl; R.sup.3 is hydrogen, hydroxy, optionally substituted alkoxy, aralkyloxy, alkanoyloxy, alkenoyloxy, cycloalkylcarbonyloxy, arylcarbonyloxy, alkoxycarbonyloxy, aralkyloxycarbonylxy, phthalidyloxy, (5-methyl-2-oxo-1,3-dioxolen-4-yl)methoxy, (5-phenyl-2-oxo-1,3-dioxolen-4-yl)methoxy, optionally substituted amino or nitro; Y is --NH-- or oxygen or sulfur; n is 1 to 5; and tautomers and salts of said compounds of formula (I), have the ability to inhibit blood platelet aggregation, and can thus be used for treatment and prophylaxis of thrombosis and embolisms.

Abstract: Compounds of formula (I): ##STR1## wherein: R.sup.1 is hydrogen, alkyl, halogen, haloalkyl, hydroxy, alkoxy, haloalkoxy, alkylthio, haloalkylthio, amino, alkanoyl, haloalkanoyl, carboxy, alkoxycarbonyl, carbamoyl, cyano, nitro, alkanesulfonyl, haloalkanesulfonyl or sulfamoyl; R.sup.2 is optionally substituted alkanoyl, optionally substituted alkenoyl, optionally substituted cycloalkylcarbonyl, substituted benzoyl, or 5,6-dihydro-1,4,2-dioxazin-3-yl; R.sup.3 is hydrogen, hydroxy, optionally substituted alkoxy, aralkyloxy, alkanoyloxy, alkenoyloxy, cycloalkylcarbonyloxy, arylcarbonyloxy, alkoxycarbonyloxy, aralkyloxycarbonylxy, phthalidyloxy, (5-methyl-2-oxo-1,3-dioxolen-4-yl)methoxy, (5-phenyl-2-oxo-1,3-dioxolen-4-yl)methoxy, optionally substituted amino or nitro; Y is --NH-- or oxygen or sulfur; n is 1 to 5; and tautomers and salts of said compounds of formula (I), have the ability to inhibit blood platelet aggregation, and can thus be used for treatment and prophylaxis of thrombosis and embolisms.