摘要:
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 agent 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-enenitrile is directly formed.
摘要:
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-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.
摘要:
2-Cyclopropyl-4-(4'-fluorophenyl)quinoline-3-carboxyaldehyde, which is useful as a starting materials for drugs, can be obtained by reacting 3-cyclopropyl-3-oxopropanenitrile with 2-amino-4'-fluorobenzophenone to thereby give 2-cyclopropyl-4-(4'-fluorophenyl)quinoline-3-carbonitrile and then reducing this product.
摘要:
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 β-ketonitrile compound, subsequently transferring the salt to an aqueous medium, and neutralizing the solution to obtain the β-Ketonitrile compound in a free state, wherein a water-incompatible organic solvent and water are added to the reaction mixture containing the β-Ketonotrile compound metal salt yielded to transfer the metal salt to the water, the resultant aqueous solution of the β-Ketonitrile compound metal salt is separated from the organic solvent by phase separation or another technique and then neutralized, and the resultant free β- Ketonitrile compound is taken out by extraction with an organic solvent.
摘要:
A process for the production of 4-aminotetrahydropyrans represented by the general formula (2) and salts thereof with acids: [wherein R is hydrogen or a hydrocarbon group], characterized by subjecting a 4-hydrazinotetrahydropyran represented by the general formula (1) or a salt thereof with an acid: [wherein R is as defined above] to decomposition in the presence of at least one compound selected from among Raney nickel, noble metal catalysts, and metal oxides; intermediates for the process; and a process for the production of the intermediates.
摘要:
A process for producing an alkyl 3-(4-tetrahydropyranyl)-3-oxopropionate compound represented by the formula (1): (1) (wherein R1 and R2 may be the same or different and each represents a group not participating in the reaction, provided that R1 and R2 may be bonded to each other to form a ring optionally containing a heteroatom therein; and R3 represents a hydrocarbon group), characterized by reacting a 4-acyltetrahydropyran represented by the formula (2): (2) (wherein R1 and R2 have the same meanings as defined above) with a carbonic diester represented by the formula (3): (3) (wherein R3 has the same meaning as defined above, provided that the two R3's may be bonded to each other to form a ring) in the presence of a base. Also provided is a process for producing the 4-acyltetrahydropyran.
摘要:
A method for producing a nitrile compound, a carboxylic acid compound or a carboxylate compound represented by the general formula (2): (2) (wherein R, R and R are as defined below) is characterized in that an acetic acid compound represented by the general formula (1) (wherein R represents a cyano group, a carboxyl group or an ester group; R and R respectively represent a group which may have a substituent and does not take part in the reaction; and R and R may combine together to form a ring) is decarboxylated in the presence of a metal catalyst.
摘要:
Quinazolin-4-one or a derivative thereof is reacted with a chlorinating agent in a first organic solvent in the presence of an organic base. Subsequently, the reaction product is reacted with an amine compound represented by the formula R5-NH-R6 (R5 and R6 each represents hydrogen or an optionally substituted hydrocarbon group) in the presence of a second organic solvent. Thus, a 4-aminoquinazoline derivative can be obtained.
摘要:
A process for producing a quinazolin-4-one derivative represented by the following formula (2): (2) (wherein R1, R2, R3, and R4 each represents a group not participating in the reaction and R1, R2, R3, and R4 may be bonded to each other to form a ring) which comprises reacting an anthranilic acid derivative represented by the following formula (1): (1) (wherein R5 represents hydrogen or a hydrocarbon group) with a formic acid derivative in the presence of an ammonium carboxylate.