112704-79-7Relevant articles and documents
Synthesis method of 2-fluoro-4-halogen benzoic acid
-
Paragraph 0033; 0036; 0054; 0057-0058, (2021/04/17)
The invention provides a synthesis method of 2-fluoro-4-halogen benzoic acid. The synthesis method comprises the following steps: (a) removing hydrogen from a substance shown in a formula (I) by using a lithium amide reagent or an alkyl lithium reagent (LDA, TMPLi, n-butyl lithium and the like), and reacting with trialkyl halosilane (TMSCl, TESCl, TBSCl and the like) to obtain a compound shown in a formula (II); (b) removing hydrogen from the compound represented by the formula (II) obtained in the step (a) by using a lithium amide reagent or an alkyl lithium reagent (LDA, TMPLi, n-butyl lithium and the like), and adding into dry ice/THF to react to obtain a compound represented by a formula (III); and (c) removing a trialkyl silane protecting group from the compound shown in the formula (III) obtained in the step (b) to obtain a compound shown in a formula (IV). According to the preparation method, starting raw materials, process routes and post-treatment processes are different, the raw materials are simple and easy to obtain, the cost is low, and the preparation method is suitable for laboratory small-scale preparation and industrial production.
Continuous synthesis method for substituted benzoic acid organic matter
-
Paragraph 0064-0066; 0138, (2019/10/01)
The invention provides a continuous synthesis method for a substituted benzoic acid organic matter. The continuous synthesis method comprises the following steps: in the presence of a catalyst and anorganic solvent, continuously putting an organic matter of a formula (I) shown in the specification, and oxygen into a continuous reaction device, carrying out a continuous oxidation reaction so as toobtain the substituted benzoic acid organic matter, and continuously discharging the substituted benzoic acid organic matter, wherein the substituted benzoic acid organic matter is of a structure ofa formula (II) shown in the specification. Oxygen is a green reagent and is cheap and easy to obtain, a great amount of wastes are not generated after reactions are completed, and the system is easy to treat. Due to continuous reaction operation, the risk that the solvent has flash evaporation explosion because of high-concentration oxygen in in-batch reactions can be reduced. Under same oxidationconditions, due to a continuous preparation process, escape of oxygen can be reduced, the utilization rate of oxygen can be greatly increased, operation can be also simplified, the security of reactions can be improved, and the yield of the substituted benzoic acid organic matter can be increased.
INHIBITORS OF STEAROYL-COA DESATURASE
-
, (2009/06/27)
Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity.
Novel 5α-reductase inhibitors: Synthesis, structure-activity studies, and pharmacokinetic profile of phenoxybenzoylphenyl acetic acids
Salem, Ola I. A.,Frotscher, Martin,Scherer, Christiane,Neugebauer, Alexander,Biemel, Klaus,Streiber, Martina,Maas, Ruth,Hartmann, Rolf W.
, p. 748 - 759 (2007/10/03)
Novel substituted benzoyl benzoic acids and phenylacetic acids 1-14 have been synthesized and evaluated for inhibition of rat and human steroid 5α-reductase isozymes 1 and 2, The compounds turned out to be potent and selective human type 2 enzyme inhibitors, exhibiting IC50 values in the nanomolar range. The phenylacetic acid derivatives were more potent than the analogous benzoic acids. Bromination in the 4-position of the phenoxy moiety led to the strongest inhibitor in this class (12; IC50 = 5 nM), which was equipotent to finasteride. Since oral absorption is essential for a potential drug, 12 was further examined. In the parallel artificial membrane permeation assay (PAMPA) it turned out to be a good permeator, whereas it was a medium permeator in Caco2 cells. After oral administration (40 mg/kg) to rats a high bioavailability and a biological half-life of 5.5 h were observed, making it a promising candidate for clinical evaluation.
Fluorine-flanked congested sites: Minimal, though perceptible buttressing effects on the proton mobility of arenes
Heiss, Christophe,Leroux, Frederic,Schlosser, Manfred
, p. 5242 - 5247 (2007/10/03)
(2,6-Difluorophenyl)trimethylsilane, -triethylsilane and -triisopropylsilane undergo sec-butyllithium-mediated metalation at the 3- and 4-position (ortho and meta relative to the halogen) in ratios of 99.6:0.4, 98:2 and 95:5, respectively. The steric pressure transmitted by the fluorine atoms can be increased if the trialkylsilyl group is locked up on the other side by a relatively voluminous substituent. Whereas (2,6-difluorophenyl)triethylsilane is attacked by lithium 2,2,6,6-tetramethylpiperidide under deprotonation of the 4- and 5-position in a ratio of 99.4:0.6, the proportion of "ortho"/ "meta" metalation changes to 84:16 when (2-bromo-6-fluorophenyl) triethylsilane acts as the substrate. Wiley-VCH Verlag GmbH & Co. KGaA, 2005.
Oxidation of toluenes to benzoic acids by oxygen in non-acidic solvents
Yang, Fan,Sun, Jing,Zheng, Rui,Qiu, Wenwei,Tang, Jie,He, Mingyuan
, p. 1225 - 1228 (2007/10/03)
Oxidation of substituted toluenes by molecular oxygen at one atmosphere to the corresponding substituted benzoic acids in non-acidic solvents was investigated. Satisfactory oxidation of halo-, methoxy-, and cyano-toluenes were achieved using Co(C18H35O2) 2/NH4Br or Co(OAc)2/NaBr/AcOH as catalysts in the presence of a radical initiator.
Amide derivative
-
, (2008/06/13)
A compound of the formula: wherein Ar is optionally substituted phenyl, etc.; n is 0, 1 or 2; R1is hydogen atom, optionally substituted alkyl, etc.; R2and R3are independently optionally substituted alkyl, etc.; R4and R5are independently hydrogen atom or optionally substituted alkyl; R6is hydrogen atom, hydroxy or alkyl; or a pharmaceutically acceptable salt thereof is useful as a medicament for treating retinal degenerative disorders and the like.
Process for the preparation of haloanthranilic acids
-
, (2008/06/13)
The present invention relates to a process for the preparation of compounds of the general formula I STR1 in which X and Y, independently of each other, represent hydrogen, fluorine, chlorine or bromine, but cannot simultaneously represent hydrogen, characterised in that compounds of the general formula II STR2 in which X and Y are defined as above, are reacted with aqueous ammonia under copper catalysis, and to intermediates for the preparation of compounds of the general formula I.
