- Novel preparation method of 3-amino-2-hydroxyacetophenone
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The invention provides a novel preparation method of 3-amino-2-hydroxyacetophenone. The novel preparation method comprises the following steps of using 2-aminophenol as an initial raw material; enabling the 2-aminophenol and acetic anhydride to synthesize 2-acetamidophenol acetate in a polar solvent under the alkaline or acid catalyzing condition; then, performing Fries rearrangement on the 2-acetamidophenol acetate in an aprotic solvent under the catalyzing action of anhydrous titanium tetrachloride, and adopting an acid hydrolysis one-pot method, so as to synthesize the 3-amino-2-hydroxyacetophenone. The novel preparation method has the advantages that the price of the used raw materials is low, the obtaining is easy, and the selection of the raw materials is diversified; the implementing of the production technology is easy, the management and control are easy, the purity of a final product is high, the dangerous technology is avoided, the equipment is simple, the synthesizing route is novel and short, the production capacity is increased, and the production and processing cost is reduced.
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Paragraph 0017; 0019
(2017/08/31)
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- Method for preparing pranlukast key intermediate 3-amino-2-hydroxyacetophenone
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The invention provides a method for preparing a pranlukast key intermediate 3-amino-2-hydroxyacetophenone. The method takes 2-aminophenol as an initial raw material, 2-aminophenol and acetic anhydride are subjected to a synthesis reaction in water to obtain 2-acetaminophenol, then 2-acetamido-4-bromophenol is prepared by 2-ace-taminophenol and NBS under room temperature, 2-hydroxy-3-amino-5-bromoacetophenone is prepared by a Hoesch reaction, finally 2-hydroxy-3-amino-5-bromoacetophenone is dissolved in ethanol, and a Pd/C is added for catalytic hydrogenation and bromine removal to obtain the 3-amino-2-hydroxyacetophenone. The raw materials have the advantages of low cost, easy acquisition, diversified raw material selection, easy realization of production technology, and easy control, the purity of the final product is high, no dangerous process is generated, the equipment is simple, the synthesis route is novel, the synthesis route is short, the production power is increased, and production processing cost is reduced.
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- New preparation method of Pranlukast
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The invention provides a new preparation method of drug Pranlukast for treating asthma. The new preparation method includes the specific steps that with 2-aminophenol-4-sulfonic acid as a starting material, a key intermediate 3-amino-2-hydroxyacetophenone is prepared by means of acylation, Fries rearrangement and deprotection, then reacts with 4-(phenylbutoxy)benzoic acid, and then is subjected to condensation with ethyl 1H-tetrazole-5-acetate, and finally preparation is achieved through ring closing under the acidic condition. Compared with the prior art, the raw material used for the new preparation method is low in price and easy to obtain, industrialization of a process can be achieved easily, and the obtained final product is high in purity; and no dangerous process exists, equipment is simple, and the route is novel.
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Paragraph 0017; 0018
(2017/05/27)
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- New preparation method of 3-amino-2-hydroxyphenylacetone
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The invention discloses a new preparation method of a key intermediate, namely 3-amino-2-hydroxyphenylacetone, for preparation of Pranlukast. The new preparation method comprises the following main steps: taking 2-aminophenol-4-sulfonic acid as a starting raw material, and carrying out acylation, Fries rearrangement, hydrolysis and deprotection, so that 3-amino-2-hydroxyphenylacetone is obtained. Compared with the prior art, the new preparation method disclosed by the invention has the advantages that the used raw materials are cheap and easily available, technology can easily realize industrialization, and the obtained final product is high in purity; no danger technology is adopted, and equipment is simple; and route is novel, and synthesis route is short.
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Paragraph 0014
(2017/08/29)
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- N-sulfamoyl-N'-benzopyranpiperidine compounds and uses thereof
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N-sulfamoyl-N′-benzopyranpiperidine compounds of formula I and their physiologically acceptable acid addition salts, pharmaceutical compositions comprising them, processes for their preparation, and their use for the treatment and/or inhibition of glaucoma, epilepsy, bipolar disorders, migraine, neuropathic pain, obesity, type II diabetes, metabolic syndrome, alcohol dependence, and/or cancer, and related concomitant and/or secondary diseases or conditions.
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Page/Page column 7
(2008/06/13)
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- N-SULFAMOYL-N’-BENZOPYRANPIPERIDINES AS INHBITORS OF CARBONIC ANHYDRASES
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The present invention relates to novel N-sulfamoyl-N'-benzopyranpiperidines of general formula (I) and their physiologically acceptable acid addition salts, to pharmaceutical compositions comprising them, processes for their preparation, and their use for the prophylaxis and/or treatment and/or prevention and/or inhibition of glaucoma, epilepsy, bipolar disorders, migraine, neuropathic pain, obesity, type II diabetes, metabolic syndrome, alcohol dependence, and/or cancer, and its concomitant and/or secondary diseases or conditions.
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Page/Page column 14
(2008/06/13)
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- Benzopyran derivatives having leukotriene-antagonistic action
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The present invention relates to novel 4-oxo-4H-1-benzopyran compounds containing benzyloxymethyl, 3-phenylpropyl, or other araliphatic substituents in their 8-position. These compounds show a leukotriene-antagonistic activity. The compounds are characterized by good oral adsorption. The compounds of the present invention may be used as anti-inflammatory and antiallergic medicaments, and in the treatment of cardiovascular diseases.
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- 2'Hydroxy tetrazole-5-carboxanilides and anti-allergic use thereof
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New tetrazole derivatives of the general formula: STR1 [wherein R1 represents a halogen atom, a straight- or branched-chain alkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl or alkylsulphamoyl group, each such group containing from 1 to 6 carbon atoms, a dialkylsulphamoyl, dialkylamino, or dialkylcarbamoyl group (wherein the two alkyl groups may be the same or different and each contains from 1 to 4 carbon atoms), a straight- or branched-chain alkanoyl, alkoxycarbonyl, alkoxycarbonylamino, alkylcarbamoyl or alkanoylamino group containing from 2 to 6 carbon atoms, a cycloalkylcarbonyl group containing from 3 to 8 carbon atoms in the cycloalkyl moiety, or a hydroxy, formyl, nitro, trifluoromethyl, trifluoroacetyl, aryl, benzyloxycarbonylamino, amino, sulphamoyl, cyano, tetrazol-5-yl, carboxy, carbamoyl, benzyloxy, aralkanoyl or aroyl group, or a group of the formula: (wherein R2 represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 5 carbon atoms, an aryl, aralkyl or trifluoromethyl group, or a cycloalkyl group containing from 3 to 8 carbon atoms, and R3 represents a hydrogen atom, or a straight- or branched-chain alkyl group containing from 1 to 6 carbon atoms optionally substituted by a phenyl group, or represents an aryl group optionally substituted by one or more substituents selected from halogen atoms and straight- or branched-chain alkyl and alkoxy groups containing from 1 to 6 carbon atoms and hydroxy, trifluoromethyl and nitro groups), and m represents zero or an integer 1, 2 or 3, the substituents R1 being the same or different when m represents 2 or 3] possess pharmacological properties, in particular properties of value in the treatment of allergic conditions.
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