- Synthetic method of fomesafen intermediate 2-chloro-4-trifluoromethylphenol
-
The invention relates to a synthetic method of fomesafen intermediate 2-chloro-4-trifluoromethylphenol. 4-(Trifluoromethyl)benzaldehyde is used as a reaction material; mCPBA (meta-chloroperoxybenzoicacid) is used as an oxidant to convert 4-(trifluoromethyl)benzaldehyde into 4-(trifluoromethyl)phenol; NCS (N-chlorosuccinimide) is used to subject 4-(trifluoromethyl)benzaldehyde to chlorination to obtain the intermediate 2-chloro-4-trifluoromethylphenol. The method has the advantages that, for instance, the materials are easy to obtain, few byproducts are produced, little pollution is caused, reaction time is short and the yield is high.
- -
-
Paragraph 0025; 0026; 0027; 0028
(2018/04/27)
-
- Method for synthesizing 2-chlorine-4-trifluoromethyl phenol
-
The invention discloses a method for synthesizing 2-chlorine-4-trifluoromethyl phenol. The method comprises the following steps: (1) carrying out an oxidation reaction, namely enabling 4-(trifluoromethyl) benzaldehyde, an organic solvent and an oxidant to react at 0 DEG C or a higher temperature in a reaction container so as to obtain 4-(trifluoromethyl) phenol; (2) carrying out a halogenation reaction, namely in the presence of an inert gas, adding a halogenation reagent and an organic solvent into another reaction container, sequentially adding a catalyst and the 4-(trifluoromethyl) phenol obtained in the step (1) at a low temperature, and stirring at a room temperature to enable the components to react, thereby obtaining 2-chlorine-4-trifluoromethyl phenol. The method is relatively highin raw material availability, relatively less in byproduct amount, low in pollution, and relatively short in reaction time, and has the characteristics that the operation is simple and convenient, products and reaction systems can be easily separated, aftertreatment is convenient and rapid, the obtained product is relatively high in purity, and the like, the yield is greatly improved, and a reliable foundation is provided for industrial production.
- -
-
Paragraph 0012; 0013; 0014; 0015
(2018/07/30)
-
- Multicomponent multicatalyst reactions (MC)2R: One-pot synthesis of 3,4-dihydroquinolinones
-
A Rh/Pd/Cu catalyst system led to an efficient synthesis of dihydroquinolinones in one-pot, two operations. The reaction features the first triple metal-catalyzed transformations in one reaction vessel, without any intermediate workup. The conjugate-addition/amidation/amidation reaction sequence is highly modular, divergent, and practical.
- Zhang, Lei,Sonaglia, Lorenzo,Stacey, Jason,Lautens, Mark
-
supporting information
p. 2128 - 2131
(2013/06/05)
-
- Syntheses and bioactivity of o- or p-trifluoromethylphenyl phosphates
-
o- and p-Trifluoromethylphenyl phosphates designed as mechanism-based phosphotyrosine phosphatase inactivators have been prepared. Some of them show herbicidal activities.
- Zhou, Xinming,He, Yantao,Wang, Miao,Ding, Yixiang
-
scheme or table
p. 651 - 659
(2009/11/30)
-
- Modular synthesis of indoles from imines and o-dihaloarenes or o-chlorosulfonates by a Pd-catalyzed cascade process
-
A detailed study of the scope of a new Pd-catalyzed synthesis of indolesfrom 1,2-dihaloarenes and o-halobenzene sulfonates and imines is descri bed. The cascade reaction comprises an imine a-arylation ollowed by an intramolecular C-N bond-forming reaction promoted by the same Pd catalyst. The reaction with 1,2-dibromobenzene shows wide scope and allows the introduction of aryl, alkyl, and vinyl substituents at different positions of the five-membered ring of the indole. The regioselective synthesis of indoles substituted in the six-membered ring can be carried out by employing o-dihalobenzene derivatives with two different halogens, taking advantage of the different reactivities of I, Br, and Cl in oxidative addition reactions. This paper also introduces a method for the efficient cleavage of the N-t-butyl group, thus allowing for the preparation of N-H indoles through the same methodology. Finally, the reaction with o-halosulfonates has been studied. The best substrates are o-chlorononaflates, which lead to indoles in very high yield. The reaction is particularlyappropriate for the synthesis of the challenging 6-substituted indoles. In view of the availability of o-chlorophenols, which are direct precur sors of the chlorononaflates, this reaction represents an efficient entry into indoles substituted in the six-membered ring. The concept is illustrated by the preparation of a 4,6-disubstituted indole from naturally occurring anethole.
- Barluenga, Jose,Jimenez-Aquino, Agustin,Aznar, Fernando,Valdes, Carlos
-
supporting information; experimental part
p. 4031 - 4041
(2009/09/04)
-
- NOVEL COMPOUNDS, ISOMER THEREOF, OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF AS VANILLOID RECEPTOR ANTAGONIST; AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME
-
This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRPV1) antagonist; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, inflammatory disease of the joints, neuropathies, HIV-related neuropathy, nerve injury, neurodegeneration, stroke, urinary bladder hypersensitivity including urinary incontinence, cystitis, stomach duodenal ulcer, irritable bowel syndrome (IBS) and inflammatory bowel disease (IBD), fecal urgency, gastro-esophageal reflux disease (GERD), Crohn's disease, asthma, chronic obstructive pulmonary disease, cough, neurotic/allergic/inflammatory skin disease, psoriasis, pruritus, prurigo, irritation of skin, eye or mucous membrane, hyperacusis, tinnitus, vestibular hypersensitivity, episodic vertigo, cardiac diseases such as myocardial ischemia, hair growth-related disorders such as effluvium, alopecia, rhinitis, and pancreatitis.
- -
-
Page/Page column 98
(2010/11/28)
-
- (2R)-2-Methylchromane-2-carboxylic acids: Discovery of selective PPARα agonists as hypolipidemic agents
-
A SAR study was conducted on chromane-2-carboxylic acid toward selective PPARα agonisim. As a result, highly potent, and selective PPARα agonists were discovered. The optimized compound 43 exhibited robust lowering of total cholesterol levels in hamster and dog animal models.
- Koyama, Hiroo,Boueres, Julia K.,Miller, Daniel J.,Berger, Joel P.,MacNaul, Karen L.,Wang, Pei-Ran,Ippolito, Marc C.,Wright, Samuel D.,Agrawal, Arun K.,Moller, David E.,Sahoo, Soumya P.
-
p. 3347 - 3351
(2007/10/03)
-
- Photochemical transformation of acifluorfen under laboratory and natural conditions
-
Acifluorfen was irradiated in pure water at various excitation wavelengths and pH values. Numerous photoproducts were obtained which were identified by [1H]NMR and /or HPLC-MS/MS. The main reaction pathways were photo-decarboxylation, photo-cleavage of the ether bonding with formation of phenolic compounds, photo-dechlorination and photo-Claisen type rearrangement. Decarboxylation was observed in acidic and neutral media whereas cleavage of the ether bonding dominated in basic media. The photo-Claisen type rearrangement only occurred on excitation at short wavelengths. The quantum yield of photolysis was significantly lower at 313nm (6.1 × 10-5) than at 254nm (2.0 × 10-3). The photoreactivity of acifluorfen was then studied in conditions approaching environmental conditions. Acifluorfen was dissolved in pure water, in water containing humic substances or in a natural water, and exposed to solar light in June at Clermont-Ferrand (latitude 46°N). In pure water, the half-life was estimated at 10 days and photo-decarboxylation accounted for 30% of the conversion. The presence of humic substances (10mg litre-1) did not affect the rate of photo-transformation. However, the half-life of acifluorfen dissolved in the natural water was only 6.8 days.
- Vialaton, Delphine,Baglio, Daniela,Paya-Perez, Ana,Richard, Claire
-
p. 372 - 379
(2007/10/03)
-
- Clorous Acid Oxidation of Trifluoromethylphenols: Cyclopentenolones by Benzilic Acid Ring Contraction
-
The formation of 2-chloro-2-trifluoromethylcyclopentane-1,3-dione (1) in the chlorous acid oxidation of 2- and 3-trifluoromethylphenol is shown to proceed via decarboxylation of 5-chloro-1-hydroxy-4-oxo-5-trifluoromethylcyclopent-2-enecarboxylic acid (4), an isolable compound.
- Blazejewski, Jean-Claude,Dorme, Regine,Wakselman, Claude
-
p. 1861 - 1864
(2007/10/02)
-
- Novel substituted phenyl ethers, process for their preparation, and their use in the preparation of substituted phenols
-
Novel compounds of the general formula STR1 in which X is hydrogen or chlorine, and each of R1, R2, R3 and R4 independently is hydrogen, methyl or ethyl, are useful intermediates in the preparation of the corresponding phenols. They may be prepared by treating a compound of the formula STR2 in which Hal is chlorine or fluorine, with a compound of the formula in the presence of a base.
- -
-
-
- 3-chloro-4-fluoro-5-nitrobenzotrifluoride
-
Chloro-aromatic compounds of the formula STR1 wherein R is CF3, OCF3, OC2 F5, CN, NCO, or COCl, m is 0, 1 or 2; n is 0, 1 or 2; q is 1 or 2; q+m+n is less than 6; and when q is 1, m is 2; are prepared by the vapor phase chloro-denitration reaction of a chlorinating agent with a nitro-aromatic compound of the formula STR2 where R, m, n and q are as defined above.
- -
-
-
- Allylthiodiphenyl ether herbicides
-
Novel allylthiodiphenyl ether compounds exhibit excellent herbicidal activity against broadleaf weeds while leaving crops such as corn, wheat, rice and soybeans unaffected. Preparation and herbicidal activity of the compounds is disclosed and exemplified.
- -
-
-
- Preparation of nuclear chlorinated aromatic compounds
-
Chloro-aromatic compounds of the formula STR1 wherein R is CF3, OCF3, OC2 F5, CN, NCO, or COCl, m is 0 or 1, and n is 0 or 1 are prepared by the vapor phase chloro-denitration reaction of a chlorinating agent with a nitro-aromatic compound of the formula STR2 where R, m, and n are as defined above.
- -
-
-
- Preparation of trifluoromethylphenyl nitrophenylethers
-
A process for preparing trifluoromethylphenyl nitro phenylethers which comprises treating a trifluoromethylhalobenzene with a base in a cosolvent system to afford a trifluoromethyl phenolate which may be isolated as its free phenol or reacted with an appropriately substituted halobenzene to afford a diphenylether herbicide or a precursor thereto.
- -
-
-
- Herbicidal 4-trifluoromethyl-4-nitrodiphenyl ethers
-
Compounds of the formula STR1 wherein X is a hydrogen atom, a halogen atom, a trihalomethyl group, an alkyl group, or a cyano group, and Y is a hydrogen atom, a halogen atom, or a trihalomethyl group, and compositions containing these compounds exhibit herbicidal activity.
- -
-
-
- Herbicidal 4-trifluoromethyl-4-nitrodiphenyl ethers
-
Compounds of the formula STR1 wherein X is a hydrogen atom, a halogen atom, a trihalomethyl group, an alkyl group, or a cyano group, and Y is a hydrogen atom, a halogen atom, or a trihalomethyl group, And compositions containing these compounds exhibit herbicidal activity.
- -
-
-