- PROCESS FOR THE PREPARATION OF 3,5-DICHLORO-2,2,2-TRIFLUOROACETOPHENONE
-
The present invention relates to an improved process for the preparation of 3,5-Dichloro-2,2,2-Trifluoroacetophenone of formula (I). The present invention further provides an improved process for the preparation of Fluralaner using 3,5-dichloro-2,2,2-trifluoroacetophenone of formula (I) obtained by a process described herein.
- -
-
Page/Page column 8-9
(2021/12/08)
-
- Preparation method of 3, 5-substituted-4-amino trifluoroacetophenone and derivatives thereof
-
The invention relates to the field of organic pharmaceutical synthesis, in particular to a preparation method of 3, 5-substituted-4-amino trifluoroacetophenone and derivatives thereof, and the preparation method of the 3, 5-substituted-4-amino trifluoroacetophenone comprises the following steps: by taking ortho-disubstituted p-aniline as a raw material, carrying out amino protection, acylation reaction and amino deprotection to obtain 4-amino trifluoroacetophenone. The reaction raw materials are simple and easy to obtain, the yield is relatively high, the reaction conditions are mild, and the method has a relatively good industrial application prospect. Besides, on the basis of the reaction, the 3, 5-substituted-4-amino trifluoroacetophenone is further subjected to amino diazotization to prepare the derivative of the 3, 5-substituted-4-amino trifluoroacetophenone, and the derivative has a relatively great application prospect in industry.
- -
-
-
- Preparation method of trifluoroacetophenone derivative
-
The invention relates to the field of organic synthesis, in particular to a preparation method of a trifluoroacetophenone derivative. Substituted aniline is used as a raw material, and preparation of the trifluoroacetophenone derivative is completed through three steps including diazotization reaction, coupling reaction and hydrolysis reaction. The preparation method has the advantages of simple process, high yield and less three wastes generated by the whole reaction, and is suitable for large-scale industrial production.
- -
-
Paragraph 0037; 0040-0041; 0046; 0048; 0052; 0066-0075; 0079
(2021/10/05)
-
- Synthesis method of 3', 5'-dichloro-2, 2, 2-trifluoroacetophenone
-
The invention relates to the technical field of chemical pharmacy, in particular to a synthesis method of 3', 5' dichloro-2, 2, 2-trifluoroacetophenone. The method comprises the following steps of: reacting 1, 3, 5-trichlorobenzene or 3, 5-dichloro-1-bromobenzene with magnesium to form a Grignard reagent, carrying out nucleophilic addition reaction on the Grignard reagent and a trifluoroacetyl reagent; and carrying out acid treatment to obtain 3', 5'-dichloro-2, 2, 2-trifluoroacetophenone; the method has the advantages of mild reaction conditions, low raw material cost, favorable economic effect and wide industrial production prospects.
- -
-
Paragraph 0025-0028; 0076
(2020/12/15)
-
- Preparation method of 3,5-dihalo trifluoroacetophenone and derivative thereof
-
The invention relates to the technical field of chemical pharmacy, particularly to a preparation method of 3,5-dihalo trifluoroacetophenone and a derivative thereof. According to the invention, , thederivatives of 3,5-dihalo trifluoroacetophenone is prepared by using 3-halogen-4-nitro trifluoroacetophenone as a raw material through reduction reaction, halogenation reaction and amino substitutionreaction, wherein the raw materials are cheap and easy to obtain, the process is simple, and the method is mild in condition, has a large-scale production prospect and has a relatively good economic effect.
- -
-
Paragraph 0024; 0026
(2020/12/31)
-
- Preparation method of 3',5'-dichloro-2,2,2-trifluoroacetophenone
-
The invention relates to the technical field of chemical pharmacy, particularly to a preparation method of 3',5'-dichloro-2,2,2-trifluoroacetophenone. According to the invention, 3',5'-dichloro-2,2,2-trifluoroacetophenone is prepared from 3'-chloro-2,2,2-trifluoroacetophenone as a raw material through four steps of nitrification, reduction, chlorination and deamination, and the method has the advantages of low raw material cost, mild reaction conditions, simple reaction process, facilitation of the reduction of the production cost, and improvement of the economic effect.
- -
-
Paragraph 0026-0053; 0060; 0063
(2020/12/31)
-
- ANTIPARASITIC COMPOUNDS
-
The present invention relates to isothiazoline compounds of formula (I). The compounds are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to a method for controlling invertebrate pests by using these compounds and to veterinary compositions comprising said compounds.
- -
-
Page/Page column 44-45
(2018/09/25)
-
- Method for preparing 3,5-dichloro-a-(trifluoromethyl)styrene
-
The invention discloses a method for preparing 3,5-dichloro-a-(trifluoromethyl)styrene (2). The method comprises the following steps: carrying out a substitution reaction on 3,5-dichlorobromobenzene used as an initial raw material and an organic fluorine
- -
-
Paragraph 0021; 0025
(2017/12/09)
-
- PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO
-
This document discloses molecules having the following formula ("Formula One"): and processes associated therewith.
- -
-
Page/Page column 47
(2014/07/08)
-
- METHOD FOR PREPARING SUBSTITUTED ISOXAZOLINE COMPOUNDS AND THEIR PRECURSORS 4-CHLORO, 4-BROMO- OR 4-IODOBENZALDEHYDE OXIMES
-
The present invention relates to a method for preparing 4-chloro-, 4-bromo- or 4- iodobenzaldehyde oximes and phenyl-substituted isoxazoline compounds prepared from these oximes.
- -
-
Page/Page column 47
(2012/05/20)
-
- PROCESS FOR PREPARING SUBSTITUTED ISOXAZOLINE COMPOUNDS AND THEIR PRECURSORS
-
Process for preparing substituted isoxazoline compounds and their precursors The present invention relates to a new method of preparing halogenated styrene compounds of Formula (VIII), which are precursors in the process of synthesis of substituted isoxazoline compounds of Formula (I), wherein R1 to R5, R8 and R9 are described as in the description. The present invention relates further to the synthesis of compounds of formula (I) starting from acetophenones. The desired styrenes of formula are prepared from the appropriate substituted acetophenone. Asides bromo anilines react with formoxime. Obtained oximes undergo a cycloaddition with the styrenes and give isoxazolines. Compounds of formula (I) can then be prepared in a palladium catalyzed carbonylative ami- nation reaction of the isoxazolines.
- -
-
Page/Page column 41
(2010/11/17)
-
- METHOD FOR PRODUCTION OF 3-HYDROXYPROPAN-1-ONE COMPOUND, METHOD FOR PRODUCTION OF 2-PROPEN-1-ONE COMPOUND, AND METHOD FOR PRODUCTION OF ISOXAZOLINE COMPOUND
-
There is provided a novel intermediate for producing pesticides. A method for producing 1,3-bis(substituted phenyl)-3-substituted-3-hydroxypropan-1-one compound of Formula (3) comprises reacting an aromatic ketone compound of Formula (4) and a substituted acetophenone compound of Formula (5) as starting raw materials in an organic solvent or water in the presence or absence of an additive in the presence of a base in a suspended state. A method for producing 1,3-bis(substituted phenyl)-3-substituted-2-propen-2-one compound of Formula (2) comprises dehydrating the compound of Formula (3). A method for producing compound (2) in one step comprises reacting compound (4) and compound (5) to obtain compound (3). Further, a method for producing an isoxazoline compound of Formula (1) comprises reacting compound (2) and a hydroxylamine in an aliphatic or an aromatic hydrocarbon solvent which is optionally substituted by a halogen atom by adding an additive selected from a phase-transfer catalyst, a C1-C6 alcohol and an aprotic polar solvent in the presence of a base and water.
- -
-
Page/Page column 73; 86
(2010/04/25)
-
- 1,3-BIS(SUBSTITUTED PHENYL)-3-HYDROXYPROPAN-1-ONE OR 2-PROPEN-1-ONE COMPOUND, AND SALT THEREOF
-
There is provided a novel process intermediate represented by the general formula (1) or (2): (where, X represents halogen atom, cyano group or the like, Y represents halogen atom, cyano group or the like, R1 represents C1-C6/s
- -
-
Page/Page column 62
(2008/12/07)
-
- Substituent Effects on the Solvolysis of 2,2,2-Trifluoro-1,1-diphenylethyl Tosylates. II. 3-Chlorophenyl- and 3,5-Dichlorophenyl-Fixed Systems
-
The solvolysis rates of 2,2,2-trifluoro-1-(3-chlorophenyl)-l-(substituted phenyl)ethyl and 2,2,2-trifluoro-1-(3,5-dichlorophenyl)-1-(substituted phenyl)ethyl tosylates or bromides were conductimetrically measured at 25.0°C in 80% aqueous ethanol. The 3-chlorophenyl-fixed series showed a bilinear Yukawa-Tsuno correlation with ρ = -4.81 and r = 1.41 for substituents more deactivating than 3,5-dimethyl, and with ρ = -6.19 and r = 1.57 for the substituent range more activating than 4-methyl. The bilinear correlation was interpreted in terms of the changing coplanarity of the two aryl rings. The 3,5-dichlorophenyl-fixed substrates gave an excellent linear Yukawa-Tsuno correlation for the substituents ranging from 4-MeO to 4-Cl with ρ = -5.95 and r = 1.69. The variable aryl rings in this series show the largest extent of resonance interaction with the extraordinary deactivated carbenium ion center by α-CF3 and α-(3,5-dichlorophenyl) groups in the transition state. The optimization of the geometries of 2,2,2-trifluoro-1,1-diphenylethyl cation and some ring-substituted derivatives was performed at the RHF/6-31G* level. The symmetric diaryl cations have equivalently twisted conformations while in unsymmetric ones the more stabilizing aryl group is less twisted from the plane of the positive sp2 carbon. The observed variation of r and ρ parameters is accommodated by geometrical changes of the incipient cation.
- Fujio, Mizue,Morimoto, Hiroshi,Kim, Hyun-Joong,Tsuno, Yuho
-
p. 3081 - 3090
(2007/10/03)
-
