- Synthesis method of 2, 4-dimethyl-3-methylsulfonylbenzoic acid
-
The invention discloses a synthesis method of 2, 4-dimethyl-3-methylsulfonylbenzoic acid. The method comprises the following steps of: nitrifying 2, 4-dimethylbenzoic acid serving as a raw material byusing concentrated nitric acid, carrying out NIS iodination, iron powder acetic acid reduction, hypophosphorous acid and sodium nitrite system deamination, carrying out methylthiolation by using dimethyl disulfide, oxidizing by using peracetic acid, extracting the reaction solution by using dichloromethane after the reaction is finished, drying, and carrying out spin-drying to obtain the target product 2, 4-dimethyl-3-methylsulfonylbenzoic acid. The method has the advantages of easily available raw materials, feasible route, simple operation, high product purity and low cost.
- -
-
Paragraph 0028-0036
(2020/06/16)
-
- Discovery of N-(3-(morpholinomethyl)-phenyl)-amides as potent and selective CB2 agonists
-
Recently sulfamoyl benzamides were identified as a novel series of cannabinoid receptor ligands. Replacing the sulfonamide functionality and reversing the original carboxamide bond led to the discovery of N-(3-(morpholinomethyl)-phenyl)-amides as potent and selective CB2 agonists. Selective CB2 agonist 31 (Ki = 2.7; CB1/CB2 = 190) displayed robust activity in a rodent model of postoperative pain.
- Worm, Karin,Weaver, Damian G.,Green, Rosalyn C.,Saeui, Christopher T.,Dulay, Doreen-Marie S.,Barker, William M.,Cassel, Joel A.,Stabley, Gabriel J.,DeHaven, Robert N.,LaBuda, Christopher J.,Koblish, Michael,Brogdon, Bernice L.,Smith, Steven A.,Dolle, Roland E.
-
scheme or table
p. 5004 - 5008
(2010/03/24)
-
- Synthesis and reactivity with β-lactamases of 'penicillin-like' cyclic depsipeptides
-
Several 7-carboxy-3-amido-3,4-dihydro-2H-1-benzopyran-2-ones have been synthesized as potential β-lactamase substrates and/or mechanism-based inhibitors. Substituted o-tyrosine precursors were prepared by the Sorensen method and then heated in vacuo to give the lactones. These compounds are cyclic analogues of aryl phenaceturates which are known to be β-lactamase substrates. The goal of incorporating the scissile ester group into a lactone was to retain the leaving group tethered to the acyl moiety at the acyl- enzyme stage of turnover by serine β-lactamases, in a manner similar to that during penicillin turnover. Further, in two cases, a functionalized methylene group para to the leaving group phenoxide oxygen was incorporated. These molecules possess a latent p-quinone methide electrophile which could, in principle, be unmasked during enzymic turnover and react with an active site nucleophile. All of these compounds were found to be substrates of class A and C β-lactamases, the first δ-lactones with such activity. Generally, k(cat) values were smaller than for the analogous acyclic depsipeptides, which suggests that the tethered leaving group may obstruct the attack of water on the acyl-enzymes. Further exploration of this structural theme might lead to quite inert acyl-enzymes and thus to significant inhibitors. Despite the apparent advantage offered by the longer-lived acyl-enzymes, the functionalized compounds were no better as irreversible inhibitors than comparable acyclic compounds [Cabaret, D.; Liu, J.; Wakselman, M.; Pratt, R. F.; Xu, Y. Bioorg. Med. Chem. 1994, 2, 757-771]. Thus, even tethered quinone methides, at least when placed as dictated by the structures of the present compounds, were unable to efficiently trap a nucleophile at serine β- lactamase active sites.
- Cabaret,Adediran,Garcia Gonzalez,Pratt,Wakselman
-
p. 713 - 720
(2007/10/03)
-
- Process for the production of nitro derivatives of aromatic compounds
-
Nitroderivates of aromatic compounds which are difficult to nitrate, can readily be obtained by nitration providing that the aromatic compound is treated with nitric acid or another nitrating agent in the presence of aliphatic or cycloaliphatic hydrocarbons monosubstituted or polysubstituted by halogen, the nitro group or an alkyl sulphonyl group, and the nitro derivative formed subsequently isolated.
- -
-
-