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: The present invention is to provide a process for preparing tetrahydropyran-4-carboxylic acid represented by the formula (1): which comprises hydrolyzing a 4-cyanotetrahydropyran-4-carboxylic acid compound represented by the formula (2): wherein R represents a hydrogen atom or a hydrocarbon group, in the presence of an acid; a process for preparing a tetrahydropyran-4-carboxylic acid ester which comprises reacting the tetrahydropyran-4-carboxylic acid represented by the above-mentioned formula (1) with an alcohol in the presence of an acid; and a process for preparing tetrahydropyran-4-carboxylic acid amide which comprises reacting the tetrahydropyran-4-carboxylic acid represented by the above-mentioned formula (1) with a halogenating agent to prepare tetrahydropyran-4-carboxylic acid halide, and then, reacting an amine compound to the resulting compound.

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: The present invention relates to a process for preparing 4-aminotetrahydropyran compound and an acid salt thereof represented by the formula (1): wherein R represents a hydrogen atom or a hydrocarbon group, which comprises subjecting a 4-hydrazinotetrahydropyran compound or an acid salt thereof represented by the formula (2): wherein R has the same meaning as defined above, to decomposition reaction in the presence of at least one compound selected from Raney nickel, a noble metal catalyst and a metal oxide, and a synthetic intermediate thereof and a process for preparing the same.

Abstract: The present invention provides a process for preparing an N,N?-dialkoxy-N,N?-dialkyl oxamide represented by the formula (3): wherein R2 and R3 may be the same or different from each other, and each represent an alkyl group having 1 to 4 carbon atoms, which comprises reacting an oxalic acid diester represented by the formula (1): wherein R1 and R1? may be the same or different from each other, and each represent a hydrocarbon group, and an N-alkyl-O-alkylhydroxylamine represented by the formula (2): R2O—NHR3 ??(2) wherein R2 and R3 have the same meanings as defined above, or an acid salt thereof in the presence of a base.

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: The present invention is to provide a process for preparing a 4-aminopyrimidine compound represented by the formula (3): wherein R1 and R2 each represent a hydrogen atom or group which does not participate in the reaction and which may have a substituent(s), and R1 and R2 may be bonded to each other to form a ring, and R4 represents a hydrogen atom or a hydrocarbon group, which comprises reacting ammonia, a 3-substituted or unsubstituted acrylonitrile compound represented by the formula (1): CR1(CN)?CR2Y??(1) wherein R1 and R2 have the same meanings as defined above, and Y represents an amino group or OR, where R represents a hydrogen atom or a hydrocarbon group, and an organic acid compound represented by the formula (2): (R3O)3CR4??(2) wherein R3 represents a hydrocarbon group, and R4 has the same meaning as defined above.

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: The present invention relates to a process for preparing tetrahydropyran-4-ol which comprises the steps of (A) a cyclization step of preparing tetrahydropyranyl-4-formate represented by the formula (1): by reacting 3-buten-1-ol, a formaldehyde compound and formic acid, and (B) then, a solvolysis step of subjecting the tetrahydropyranyl-4-formate to solvolysis to obtain tetrahydropyran-4-ol represented by the formula (2): and an intermediate and a process for preparing the same.

Abstract: The present invention discloses a process for preparing a nitrile compound, a carboxylic acid compound or a carboxylic acid ester compound represented by the formula (2): wherein R represents a cyano group, a carboxyl group or an ester group, R1 and R2 each represent a group which does not participate in the reaction, which may have a substituent, and R1 and R2 may be combined to each other to form a ring, which comprises subjecting an acetic acid compound represented by the formula (1): wherein R, R1 and R2 have the same meanings as defined above, to decarboxylation in the presence of a metal catalyst.

Abstract: A dibenzothiazepine compound is suitably prepared by subjecting a 2-amino-2?-carboxy-diphenylsulfide compound to dehydration-condensation reaction in the presence of an acidic catalyst; the 2-amino-2?-carboxy-diphenylsulfide compound is suitably prepared by reducing a 2-nitro-2?-carboxy-diphenylsulfide compound in a lower aliphatic ester solvent; and the 2-nitro-2?-carboxy-diphenylsulfide compound is suitably prepared by reacting a nitrobenzene compound with a thiosalicylic acid compound in a mixture of a lower aliphatic alcohol and water.

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 relates to a process for preparing 4-aminotetrahydropyran compound and an acid salt thereof represented by the formula (2): wherein R represents a hydrogen atom or a hydrocarbon group, which comprises subjecting a 4-hydrazinotetrahydropyran compound or an acid salt thereof represented by the formula (1): wherein R has the same meaning as defined above, to decomposition reaction in the presence of at least one compound selected from Raney nickel, noble metal catalyst and metal oxide, and a synthetic intermediate thereof and a process for preparing the same.

Abstract: The present invention provides a process for preparing an N,N?-dialkoxy-N,N?-dialkyl oxamide represented by the formula (3): wherein R2 and R3 may be the same or different from each other, and each represent an alkyl group having 1 to 4 carbon atoms, which comprises reacting an oxalic acid diester represented by the formula (1): wherein R1 and R1? may be the same or different from each other, and each represent a hydrocarbon group, and an N-alkyl-O-alkylhydroxylamine represented by the formula (2): R2O—NHR3??(2) wherein R2 and R3 have the same meanings as defined above, or an acid salt thereof in the presence of a base.

Abstract: The present invention relates to a process for preparing tetrahydropyran-4-one represented by the formula (1): which comprises reacting at least one kind of dihydropyran-4-one and pyran-4-one represented by the formula (2): wherein represents a single bond or a double bond, and hydrogen (a) in the presence of a metal catalyst, in a mixed solvent of an aprotic solvent and an alcohol solvent, or (b) in the presence of an anhydrous metal catalyst in which a hydrated metal catalyst is subjected to dehydration treatment, in a hydrophobic organic solvent.

Abstract: The present invention is to provide a process for preparing an alkyl 3-(4-tetrahydropyranyl)-3-oxopropanoate compound represented by the formula (1): wherein R1 and R2 may be the same or different from each other, and represent a group which does not participate in the reaction, and R1 and R2 may be bonded to form a ring, and the ring may contain a hetero atom(s), and R3 represents a hydrocarbon group, which comprises reacting 4-acyltetrahydropyran represented by the formula (2): wherein R1 and R2 have the same meanings as defined above, and a carbonic acid diester represented by the formula (3): wherein R3 has the same meanings as defined above, and two R3s may be bonded to each other to form a ring, in the presence of a base, and a process for preparing 4-acyltetrahydropyran.

Abstract: The present invention discloses a process for preparing a nitrile compound, a carboxylic acid compound or a carboxylic acid ester compound represented by the formula (2): wherein R represents a cyano group, a carboxyl group or an ester group, R1 and R2 each represent a group which does not participate in the reaction, which may have a substituent, and R1 and R2 may be combined to each other to form a ring, which comprises subjecting an acetic acid compound represented by the formula (1): wherein R, R1 and R2 have the same meanings as defined above, to decarboxylation in the presence of a metal catalyst.

Abstract: A process comprising a reaction of ethyl 2-amino-4,5-bis(2-methoxyethoxy)benzoate with a formic acid compound in the presence of an ammonium carboxylate gives 6,7-bis(2-methoxyethoxy)quinazolin-4-one in a high yield.

Abstract: A pyrimidin-4-one compound can be prepared in a high yield by reacting an aminoarylcarboxylic acid compound with an organic acid compound in the presence of a nitrogen atom-containing compound under relatively simple and moderate reaction conditions.

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.