- Preparation method of 3-carboxybenzaldehyde
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The invention discloses a preparation method of 3-carboxybenzaldehyde. The method comprises the following steps: by using m-toluonitrile as a starting raw material, carrying out a first hydrolysis reaction, and adding an acid to carry out an acidification reaction to obtain m-toluic acid; carrying out chlorination reaction on m-toluic acid to obtain 3-carboxyl benzyl chloride; mixing the 3-carboxyl benzyl chloride and urotropin for an oxidation reaction, then adding glacial acetic acid and water for a second hydrolysis reaction to obtain the 3-carboxybenzaldehyde. According to the method disclosed by the invention, m-toluonitrile with low cost is used as a raw material, the 3-carboxybenzaldehyde is synthesized through a series of processes of hydrolysis, chlorination, oxidation and hydrolysis, and the product purity and yield are relatively high; the method has the advantages of simple and safe process operation, easily available raw materials and low cost and is suitable for industrial production.
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Paragraph 0040; 0042; 0045; 0047; 0050; 0052
(2020/04/29)
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- 3-chloro methyl benzoic acid synthetic method
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The present invention relates to a 3-chloro methyl benzoic acid synthetic method, and the specific method is as follows: in zinc chloride, ferric chloride and other Lewis acid catalysts, 3-chloro methyl benzoic acid is synthesized from benzoyl chloride and paraformaldehyde in a solvent in one step. The synthetic method is a one-step reaction, and is simple and easy to control, highly-safe, and high in finished product yield, starting materials are cheap and readily available, the synthetic method is less in waste, the waste can be harmlessly processed, and the synthetic method is clean and environmentally-friendly, and the purity of the 3-chloro methyl benzoic acid prepared by the synthetic method is high.
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Paragraph 0034; 0035
(2016/10/10)
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- N-Cycloalkanoyl-L-phenylalanine derivatives as VCAM/VLA-4 antagonists.
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A systematic structure-activity relationship investigation of the lead compound 1 resulted the identification of several N-[(substituted alkyl)cycloalkanoyl]-4-[((2,6-dichlorophenyl)carbonyl)amino]-L-phenylalanine derivatives as potent VCAM/VLA-4 antagonists. The data are consistent with a model of these compounds in which these alkanoylphenylalanines reside in a compact gauche (-) bioactive conformation.
- Sidduri, Achyutharao,Tilley, Jefferson W,Hull, Kenneth,Lou, Jian Ping,Kaplan, Gerry,Sheffron, Allen,Chen,Campbell, Robert,Guthrie, Robert,Huang, Tai-Nan,Huby, Nicholas,Rowan, Karen,Schwinge, Virginia,Renzetti, Louis M
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p. 2475 - 2478
(2007/10/03)
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- N-alkanoylphenylalanine derivatives
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Compounds of the formula: are disclosed which have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4. Such compounds are useful for treating diseases whose symptoms and/or damage are related to the binding of VCAM-1 to cells expressing VLA-4.
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- Process for the solubilization of peptides and process for peptide synthesis
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A process is disclosed for making peptides soluble in a water-immiscible organic solvent, comprising linking a lipophilic group with an amide or ester bond to the terminal carboxyl group of said peptide; when the lipophilic group is linked to L-serine, a molecule is obtained with a solubility in water at 25° C. of less than 30 g/liter. This lipophilic group is non-polymeric and chemically defined. A process is also disclosed for the synthesis of peptides, optionally protected, in a liquid medium, wherein the starting material is an amino acid or peptide made soluble in an organic medium by a lipophilic group A--L linked to the carboxyl function of the starting amino acid or peptide, and are added to amino acids or peptides to be condensed which are activated on their acid function and protected on their amine function and are optionally protected on their side chain. The peptides resulting from the synthesis are used, where appropriate, for the synthesis of medicinal products, vaccines or agri-foodstuff or plant-protection.
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- Oxidation of Aromatic Compounds. II. Oxidation of Methyl Derivatives of Benzoic Acid and Acetophenone in the System HSO3F-PbO2
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Low-temperature oxidation of methyl derivatives of benzoic acid and acetophenone in the system HSO3F-PbO2 proceeds with intermediate formation of radical cations and results in replacement of hydrogen atom in methyl group or benzene ring.The reaction allows preparation of various substituted derivatives of benzyl alcohols and alkylated phthalides.
- Rudenko, A. P.,Korovina, N. S.
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p. 1084 - 1088
(2007/10/03)
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- THE ESR SPECTRA, STRUCTURE, AND REACTIVITY OF AROMATIC RADICAL-CATIONS IN SUPERACIDS
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The oxidation of aromatic compounds by lead dioxide in superacids based on fluorosulfonic acid at -75 deg C takes place by a one-electron mechanism and leads in many cases to relatively stable radical-cations.The ESR spectra, the isotropic hyperfine coupling constants, data on the reactivity of the radical-cations, and the structures of the final products from their transformations under "long-life" conditions are presented.
- Rudenko, A. P.
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p. 1946 - 1980
(2007/10/03)
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