2252-51-9Relevant articles and documents
Stepwise benzylic oxygenation via uranyl-photocatalysis
Hu, Deqing,Jiang, Xuefeng
supporting information, p. 124 - 129 (2022/01/19)
Stepwise oxygenation at the benzylic position (1°, 2°, 3°) of aromatic molecules was comprehensively established under ambient conditions via uranyl photocatalysis to produce carboxylic acids, ketones, and alcohols, respectively. The accuracy of the stepwise oxygenation was ensured by the tunability of catalytic activity in uranyl photocatalysis, which was adjusted by solvents and additives demonstrated through Stern–Volmer analysis. Hydrogen atom transfer between the benzylic position and the uranyl catalyst facilitated oxygenation, further confirmed by kinetic studies. Considerably improved efficiency of flow operation demonstrated the potential for industrial synthetic application.
Chlorobenzene-pyridine compounds and application thereof
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Paragraph 0099; 0101; 0102; 0103, (2018/04/01)
The invention relates to chlorobenzene-pyridine compounds and an application thereof. The compounds can be used for preparing a Smoothened protein inhibitor and a drug for resisting adenocarcinoma andesophagus cancer and have the structure in the general formula (I) shown in the description, wherein X is selected from the structure shown in the description, R1 is selected from H or the structureshown in the description, and R2 is selected from the structure shown in the description.
2-chloro-4-fluorobenzoic acid and preparation method thereof
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Paragraph 0041-0042, (2017/04/03)
The invention discloses 2-chloro-4-fluorobenzoic acid and a preparation method thereof. With m-chloroaniline as a raw material, the method comprises the following steps: realizing amino protection through 2-(trimethylsilyl) ethoxymethyl chloride; realizing formylation through a Vilsmeier-Haack reaction; oxidizing to obtain carboxylic acid; performing hydrogenation reduction of nitro; and performing a fluorination reaction to obtain 2-chloro-4-fluorobenzoic acid. The pesticide intermediate 2-chloro-4-fluorobenzoic acid disclosed by the invention is easy to prepare and suitable for batch production; and moreover, by adopting the cheap m-chloroaniline as a raw material and the substances with low volatility and low toxicity in the preparation process and by controlling the types and addition amount of the catalyst and oxidant, the product yield is more than or equal to 85%.
Flow carbonylation of sterically hindered ortho-substituted iodoarenes
Mallia, Carl J.,Walter, Gary C.,Baxendale, Ian R.
supporting information, p. 1503 - 1511 (2016/08/02)
The flow synthesis of ortho-substituted carboxylic acids, using carbon monoxide gas, has been studied for a number of substrates. The optimised conditions make use of a simple catalyst system compromising of triphenylphosphine as the ligand and palladium acetate as the pre-catalyst. Carbon monoxide was introduced via a reverse "tube-in-tube" flow reactor at elevated pressures to give yields of carboxylated products that are much higher than those obtained under normal batch conditions.
INHIBITORS OF STEAROYL-COA DESATURASE
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, (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.
Process for the preparation of halogenated benzoic acids
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, (2008/06/13)
A process for the preparation of halogenated benzoic acids of formula (1): STR1 in which R1, R2, R3, R4 and R5 are hydrogen, fluorine, chlorine or bromine atoms or C1 -C6 -alkyl, C1 -C6 -alkoxy, nitro, cyano, trifluoromethyl, aidehyde, C1 -C4 -alkoxycarbonyl, -SO2 -C1 -C4 -alkyl, -SO2 -phenyl, -CONH2, -CON(C1 -C4 -alkyl)2, hydroxy, carboxy, -NH2 or -N(C1 -C4 - alkyl)2 groups, at least one of the substituents R1 -R5 being one of said halogen atoms, which comprises reacting 1 mol of a benzophenone, asymmetrically substituted on the benzene rings A and B, of general formula (2): STR2 in which R1 -R10 are as defined above for R1 -R5, with about 1 to about 10 mol of an oxidizing agent selected from the group comprising hydrogen peroxide, urea/hydrogen peroxide addition product, an alkali metal peroxide, ammonium, alkali metal or alkaline earth metal peroxodisulfates, pertungstates, perborates or percarbonates, ozone, alkyl- or aryl-percarboxylic acids, alkyl- or aryl-persulfonic acids or persulfuric acid, at temperatures from about -20° to about +100° C.
Novel N-imides
Wheeler, Thomas N.,Craig, Todd A.,Morland, Robert B.,Ray, John, A.
, p. 883 - 887 (2007/10/02)
A convenient method for the synthesis of N--3,4,5,6-tetrahydrophthalimides using benzyl triflates is described.
Synthesis of α methyl 4 (2 thienylcarbonyl)benzeneacetic acid, suprofen, and derivatives
van Daele,Boey,Sipido,De Bruyn,Janssen
, p. 1495 - 1501 (2007/10/05)
A series of compounds with general structure Het CO Ar CH(CH3)COOH was prepared for pharmacological screening. Different synthetic approaches are described. α Methyl 4 (2 thienylcarbonyl)benzeneacetic acid (compound III-l, suprofen), was found to show a marked antiwrithing activity. Furthermore this compound proved to be a potent inhibitor of prostaglandin biosynthesis.
