KR840008326A - Process for preparing pyrazolone derivative-containing pharmaceuticals - Google Patents

Abstract

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Description

Process for preparing pyrazolone derivative-containing pharmaceuticals

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Claims (1)

The hydrazine of general formula (II) is reacted with a β-keto acid derivative of general formula (III) at 10 to 200 ° C. in the presence of an inert solvent and a basic or acidic catalyst if necessary, or a compound of general formula (IV) The pyrazol-5-one derivative of formula (V) and, if necessary, are reacted at 10 to 200 ° C in the presence of an inert solvent and an inorganic or organic base, or the acetylene carboxylic acid derivative of formula (VI) is Reacting the hydrazine with, if necessary, in the presence of an inert solvent and an inorganic or organic base at 50 to 200 ° C, or the compound of general formula (IX) is an acid derivative, preferably a carboxylic acid or carboxylic acid derivative of general formula (VII) or a general formula The sulfonic acid derivative of (VIII) is reacted at -20 to 150 DEG C in the presence of an inert solvent and basic additive or organic base if necessary to prepare a compound of formula (I), and then the compound of formula (I) cure Appropriate effective amounts are mixed with pharmaceutically acceptable diluents or excipients and prepared in suitable dosage forms, characterized by salts and pulmonary shock and lipoxygenase-inhibitors, anti-allergic agents, anti-allergic agents, anti-inflammatory agents in skin and eye A method of making a medicament useful as an asthma, anti-nausea, antiarrhythmic, anti-edema, bronchial dilator and gastroprotective agent. In the general formula, R is an aryl or heteroaryl group having 6 to 12 carbon atoms [these are halogen, trifluoromethyl, alkyl, alkenyl, alkoxy, alkylamino, cyano, trifluoromethoxy, nitro, hydroxyl, SOn- The same or different 1 to 3 substituents selected from alkyl, wherein n is 0 to 2 or SOn-trifluoromethyl, wherein n is 0 to 2, wherein in each case alkyl, alkenyl and alkoxy are 1 Optionally containing from 4 to 4 carbon atoms; and R ³ is hydrogen; Or a hydrocarbon group of 1 to 18 carbon atoms, optionally containing 1 to 8 carbon atoms, optionally containing hydroxyl, ether, ester or carboxyl groups, and optionally containing 1 to 3 halogen atoms, and R ² is the same as R ¹ Or the following general formula R ³ is hydrogen, an acyl of 1 to 15 carbohydrates or a sulfonyl group of 1 to 15 carbon atoms, and X is —CH ₂ —CH ₂ —CH ₂ —, —O—CH ₂ —CH ₂ —, —S—CH ₂ -CH _2- , -CH ₂ -CH _2- , or One of the groups, wherein an oxygen or sulfur atom is bonded to the R group, provided that when R is β-naphthyl, R ¹ is CH ₃ and R ² and R ³ are hydrogen, X is —O—CH ₂ − Is not CH _2- , Y is a leaving group such as hydroxyl, alkoxy, aralkoxy, amino or alkylamino group, and A is a halogen, dialkyloxonium, dialkylsulfonium or trialkylammonium group, or aryl- or trifluor A leaving group such as a chlorosulfonic acid group, A 'is a halogen, a 5-membered heterocyclic azole ring, an alkyl group bonded to a carbonyl carbon by oxygen or a sulfur atom, a phenyl group optionally substituted with one or two nitro groups, or A leaving group such as an acyloxy group, R ⁴ -C═O and R ⁵ -SO ₂ have the same meaning as R ³ and A ′ is halogen. ※ Note: The disclosure is based on the initial application.