摘要:
A NK1 antagonist having the formula (I), with the variables defined herein, which is useful for treating a number of disorders, including emesis, depression, anxiety and cough.
摘要:
A process for the preparation of compounds of general formula (III) or salts thereof wherein R1 is a heterocyclic group or the like; X is -CO- or the like; n is 1 to 3; Y is oxygen or the like; A is a benzene ring or the like; p is 1 to 8; R2 is a heterocyclic group or the like; q is 0 to 6; m is 0 or 1; R?4 and R5¿ are each a hydrocarbon group or the like; or alternatively R?4 and R2¿ may be united to form a ring), characterized by reacting a compound of general formula (I) or a salt thereof (wherein Z is halogeno or the like) with a compound of the general formula (II) or a salt thereof in an amide in the presence of a metal alkoxide.
摘要:
The invention relates to a method for producing vinyl oxime-ethers of general formula (I) by reacting an oxime with an alkine, where R?1 and R2¿ are the same or different and represent alkyl or aryl rests, R3 is hydrogen, an alkyl or aryl rest, and R4 is a rest which is the same as R3 and can be different from R3 or represents a hydroxy alkyl rest. According to the invention the reaction is carried out in a superbasic, polar organic solvent in the presence of a strong base, under conditions which are such that the resulting vinyl oxime-ether remains in contact with the other constituents of the reaction mixture for such a short time that it cannot to a significant extent convert into secondary products or decompose.
摘要:
Methoxyiminoacetamide derivatives represented by general formula (I), exhibiting negative specific rotations in chloroform, and having an extremely excellent pesticidal activity, wherein Ar is aryl or heteroaryl; Y is hydrogen, halogeno, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkylthio, C2-C6 alkynyloxy, cyano, nitro or aryl; and n is an integer of 1 to 3.
摘要:
The method for producing the benzyl bromide derivatives of the formula: wherein R 1 represents a C 1 to C 5 alkyl group, which comprises reacting a 2-methylphenylacetic acid derivative of the formula: wherein R 1 represents the same meaning above, with bromine in the presence of an alkali metal salt. In case that R 1 is an ethyl or isopropyl group, the recrystallization of the above reaction product from aliphatic hydrocarbon solution gives the benzyl bromide derivatives efficiently and in high purity.
摘要:
A process for producing a carboxylic acid derivative represented by general formula [VIII], (wherein R , R , R and L are each as defined in the specification), which comprises reacting a benzyl halide with a cyano compound to give a phenylacetonitrile, reacting the nitrile with an alkyl nitrite in the presence of a base to give an alpha -hydroxyiminophenylacetonitrile, reacting the hydroxy nitrile with an alkylating agent to give an alpha -alkoxyiminophenylacetonitrile, hydrolyzing the alkoxy nitrile in the presence of a base, optionally after hydration and acid treatment, to give an alpha -alkoxyiminophenylacetic acid, and finally reacting the acid with a halogenating agent, or converting the acid into a corresponding metal salt and reacting the salt with an alkylating agent, or reacting the acid with a lower alcohol in the presence of an acidic catalyst. According to this process, the reactions can be advanced through the respective steps under mild conditions, and the target derivative [VIII] can be produced even without resort to high-pressure steam equipment, high-temperature heat medium equipment, refrigerator, and so forth. Further, this process is advantageous in that only a single solvent will suffice without the necessity for using various solvents according to the respective steps.
R¹ für C₃-C₆-Alkenyl, für gegebenenfalls durch C₁-C₄-Alkyl substituiertes C₃-C₆-Cycloalkyl, für C₁-C₆-Alkoxy, für C₁-C₄-Alkylamino oder für Di-(C₁-C₄-alkyl)-amino steht und R² für Fluor, Chlor, Brom oder Jod steht, sind Ausgangs- bzw. Zwischenprodukte für die Herstellung von halogenierten Sulfonylaminocarbonyltriazolinonen mit herbizider Wirksamkeit.