摘要:
The purpose of the present invention is to provide an economically favorable, industrialization-suitable method for manufacturing nitrobenzene compounds of general formula (1). A method for manufacturing nitrobenzene compounds of general formula (1):
(in the formula, R 1 represents a halogen atom; R 2 , R 3 , and R 4 represent a hydrogen atom, etc.; and R 5 represents a halogen atom or alkoxy carbonyl group), the method including the following processes: (i) a process for reacting aniline compounds of general formula (2):
(in the formula, R 1 , R 2 , R 3 , R 4 , and R 5 are as previously defined.) in the presence of a metal salt of nitrous acid and an acid, and (ii) a process for reacting the product of process (i) in the presence of a metal salt of nitrous acid and a copper compound; and the total amount of water used in process (ii) being 1.2-2.2 L (liters) with respect to one mole of the compound of general formula (2).
摘要翻译:本发明的目的是提供一种经济上有利的工业化合适的制备通式(1)的硝基苯化合物的方法。 制备通式(1)的硝基苯化合物的方法:(式中,R 1表示卤素原子; R 2,R 3和R 4表示氢原子等; R 5表示卤素原子或 烷氧基羰基),该方法包括以下方法:(i)使通式(2)的苯胺化合物反应的方法:(式中,R 1,R 2,R 3,R 4和R 5为 (ii)在亚硝酸金属盐和铜化合物的存在下使方法(i)的产物反应的方法;和(ii)使方法(i)的产物在亚硝酸金属盐和铜化合物的存在下反应的方法; 并且相对于1摩尔通式(2)的化合物,方法(ii)中使用的水的总量为1.2-2.2L(升)。
摘要:
The present invention relates to a process for producing substituted biphenyls by reacting aryl halides with tetraarylborates in the presence of palladium catalysts.
摘要:
The present invention provides an efficient, safe and cost effective way to prepare 5-(4-methyl-1 H -imidazol-1-yl)-3-(trifluoromethyl)-benzenamine which is a key intermediate for the preparation of substituted pyrimidinylaminobenzamides of formula (II):
摘要:
The invention relates to a method for producing substituted biphenyls of formula (I), wherein R 1 = nitro or amino, R 2 = cyano, halide, C 1 -C 4 alkyl halide, C 1 -C 4 alkoxy halide or C 1 -C 4 alkylthio halide, n = 0 to 3 and R 3 = hydrogen, cyano or halide, characterized by reacting a halobenzene of formula (Il), wherein HaI represents chlorine or bromine, with a phenyl boronic acid (IVa) of a diphenyl borinic acid (IVb) or a mixture of (IVa) and (IVb) in a solvent or diluent in the presence of a base and of a palladium catalyst which consists of palladium and a bidentate phosphorus ligand of formula (III), wherein Ar represents optionally substituted phenyl and R 4 and R 5 represent C 1 -C 8 alkyl or C 3 -C 6 cycloalkyl each or together form a two- to seven-membered bridge which can optionally carry a C 1 -C 6 alkyl substituent.
摘要:
The invention relates to a fungicidally active compound of formula (I): where Het is a 5- or 6-membered heterocyclic ring containing one to three heteroatoms, each independently selected from oxygen, nitrogen and sulphur, the ring being substituted by the groups R6, R7 and R8; R1 is hydrogen, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, C1-4 haloalkoxy, CH2C≡CR9, CH2CR10=CHR11, CH=C=CH2 or COR12; R2 and R3 are each, independently, hydrogen, halo, C1-4 alkyl, C1-4 alkoxy, C1-4 haloalkyl or C1-4 haloalkoxy; R4 and R5 are each independently selected from halo, cyano and nitro; or one of R4 and R5 is hydrogen and the other is selected from halo, cyano and nitro; R6, R7 and R8 are each, independently, hydrogen, halo, cyano, nitro, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy(C1-4)alkyl, C1-4 haloalkoxy(C1-4)alkyl or C1-4 haloalkoxy, provided that at least one of R6, R7 and R8 is not hydrogen; R9, R10 and R11 are each, independently, hydrogen, halo, C1-4 alkyl, C1-4 haloalkyl or C1-4 alkoxy(C1-4)alkyl; and R12 is hydrogen, C1-6 alkyl, C1-6 haloalkyl, C1-4 alkoxy(C1-4 )alkyl, C1-4 alkylthio(C1-4)- alkyl, C1-4 alkoxy or aryl; to the preparation of these compounds, to novel intermediates used in the preparation of these compounds, to agrochemical compositions which comprise at least one of the novel compounds as active ingredient, to the preparation of the compositions mentioned and to the use of the active ingredients or compositions in agriculture or horticulture for controlling or preventing infestation of plants by phytopathogenic microorganisms, preferably fungi.
摘要:
Disclosed are processes for the preparation of 2-substituted indole compounds wherein the 2-substituent comprises an R4 group, wherein R4 is selected from the group consisting of monocyclic aromatic, polycyclic aromatic, monocyclic heteroaromatic, polycyclic heteroaromatic, 1° alkyl, and alkenyl, all of which are optionally substituted at one or more substitutable positions with one or more suitable substituents, and wherein R4 is bonded to the 2-position of the indole ring via a C-C bond; the process comprising reacting an orthogem-dihalovinylaniline compound of the formula (I): wherein Halo comprises Br, Cl, or I; each of the one or more R1 is independently selected from the group consisting of H, fluoro, lower alkyl, lower alkenyl, lower alkoxy, aryloxy, lower haloalkyl, lower alkenyl, -C(O)O-lower alkyl, monocyclic or polycyclic aryl or heteroaryl moiety, or R1 is an alkenyl group bonded so to as to form a 4- to 20-membered fused monocycle or polycyclic ring with the indole ring; all of which are optionally substituted with one or more suitable substituents at one or more substitutable positions; R2 comprises H, alkyl, cycloalkyl, aryl, heteroaryl, aryl-loweralkyl-, or heteroaryl-loweralkyl-, all of which are optionally substituted at one or more substitutable positions with one or more suitable substituents; R3 comprises H, alkyl, haloalkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, heterocycle, aryl-(C1-6)alkyl-, or heteroaryl-loweralkyl-, all of which are optionally substituted at one or more substitutable positions with one or more suitable substituents; with an organoboron reagent selected from the group consisting of a boronic ester of R4, a boronic acid of R4, a boronic acid anhydride of R4, a trialkylborane of R4 and a 9-BBN derivative of R4; in the presence of a base, a palladium metal pre-catalyst and a ligand under reaction conditions effective to form the 2-substituted indole compound. Also disclosed are processes for the preparation of ortho-gem-dihalovinylaniline compounds. Novel compounds prepared by the processes and novel uses of the compounds are likewise disclosed.
摘要:
The invention relates to a method for preparation of fluorinated aromatic compounds from the corresponding amines by replacement of the amino group with a fluorine atom. The method of preparation of a fluoroaromatic compound from an aromatic compound with at least one amino group on the aromatic ring is characterized by the reaction of said aromatic amine compound with a nitrosating agent in the presence of a source of boron trifluoride in an organic medium, and carrying out a thermal treatment of the reaction medium comprising the diazonium salt thus obtained to give the fluoroaromatic compound directly by decomposition of the diazonium salt without intermediate isolation thereof.