KR860002495A - Method for preparing novel pyridylethyl-dihydropyridine - Google Patents

Abstract

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Description

Method for preparing novel pyridylethyl-dihydropyridine

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Claims (10)

Pyridylethyl-dihydropyridine and its physiologically acceptable salts thereof represented by the following general formula (I). Wherein R ¹ is hydrogen or a straight or branched chain alkyl group, which alkyl group is optionally substituted by halogen, nitro, cyano, carboxyl, carboxamido, alkoxy or alkoxycarbonyl, and R ² and R ³ Are the same or different from each other and are hydrogen, or a straight or branched chain alkyl group (this alkyl group is optionally substituted by halogen, aryl, carboxyl, alkoxy or alkoxycarbonyl), or R ² is bonded to X (or) R ³ is bonded to Y to form a five or six membered ring, X and Y being the same or different from each other, hydrogen, cyano or Where Z is a direct bond or is oxygen, sulfur or NH, R ⁴ is or a straight or branched chain alkyl group, which alkyl group is halogen, nitro, pyridyl, cyano, amino, carboxyl, alkoxy or alkoxy Optionally substituted with carbonyl). The compound of claim 1, wherein R ¹ is hydrogen or a linear branched alkyl group [This alkyl group has a maximum of 6 carbon atoms, and fluorine, chlorine, bromine, carboxyl or alkoxy or alkoxycarbonyl (in each case, the alkoxy group is Optionally substituted with up to 6 carbon atoms), and R ² and R ³ are the same or different from each other, and hydrogen or a straight or branched chain alkyl group [the alkyl group has up to 6 carbon atoms, fluorine, Chlorine, bromine, aryl (6-10 carbon atoms), carboxyl, or alkoxy or alkoxycarbonyl (in each case, an alkoxy group is optionally substituted with up to 6 carbon atoms), or a single bond And combine with X and / or Y to form a five-membered or six-membered ring, wherein X and Y are the same or different from each other and are hydrogen, cyano or Wherein Z is a direct bond or is oxygen, sulfur or NH, R ⁴ is hydrogen or a straight or branched chain alkyl group which has up to 6 carbon atoms, fluorine, chlorine, bromine, nitro, Pyridylethyl-dihydro of formula (I) wherein pyridyl, cyano, amino, carboxyl, or alkoxy or alkoxycarbonyl in each case is optionally substituted by 6 carbon atoms Pyridine and its physiologically acceptable salts. The compound of claim 1, wherein R ¹ is hydrogen or a straight or branched alkyl group [This alkyl group has a maximum of four carbon atoms, and carboxyl or alkoxy or alkoxycarbonyl (in each case, the alkoxy group has a maximum of four carbon atoms) Optionally substituted] and R ² and R ³ are the same as or different from each other, and hydrogen or a straight or branched chain alkyl group having up to 4 carbon atoms, and fluorine, chlorine, bromine, phenyl, car Carboxyl or alkoxycarbonyl, wherein the alkoxy group is optionally substituted by up to 4 carbon atoms, or combines with X and / or Y by a single bond to form a 5 or 6 membered ring, X and Y are the same as or different from each other, and hydrogen, cyano or Wherein Z is a direct bond or is oxygen or NH, R ⁴ is hydrogen or a straight or branched chain alkyl group, the alkyl group having up to 4 carbon atoms, fluorine, chlorine, bromine, cyano, pyri Diyl, amino, carboxyl or alkoxy or alkoxycarbonyl) in each case, the alkoxy group is optionally substituted by up to 4 carbon atoms) and pyridylethyl-dihydropyridine of formula (I) and physiological Its salts, academically acceptable. In the method for producing a compound represented by the following general formula (I), [Wherein R ¹ is hydrogen or a linear or branched alkyl group (this alkyl group is optionally substituted by halogen, nitro, cyano, carboxyl, carboxamido, alkoxy or alkoxycarbonyl group), R ² and R ³ Are the same or different from each other and are hydrogen, or a straight or branched chain alkyl group, which alkyl group is optionally substituted by halogen, aryl, carboxyl, alkoxy or alkoxycarbonyl group, or by a single bond with X and / or Y Combine to form a five or six membered ring, X and Y being the same or different from each other, hydrogen, cyano or Wherein Z is a direct bond or is oxygen, sulfur or NH, and R ⁴ is hydrogen or a straight or branched chain alkyl group which is halogen, nitro, pyridyl, cyano, amino, carboxyl, alkoxy or Optionally substituted with an alkoxycarbonyl group). (A) Enamine of the following general formula (II) Wherein R ¹ , R ² and X are as defined above, but X and R ⁴ are not hydrogen. Keto compound of formula (III) in the presence of an inert organic solvent, if necessary. (Wherein R ³ and Y are as defined above, Y and R ⁴ are not hydrogen) and the aldehyde of formula (IV) React with, or (B) Keto compound of general formula (III) (a, b). Wherein R ² , R ³ , X and Y are as defined above, but X, Y and R ⁴ are not hydrogen) When R ³ and R ² and / or X and Y are different from each other, if necessary, in the form of a mixture of the same amount, in the presence of an inert organic solvent, if necessary, the aldehyde of the formula (IV) and the following general formula Amine of (V) R ¹ -NH ₂ (Ⅴ) Wherein R ¹ is as defined above Or after reacting with a salt thereof, if necessary, a compound of formula (I) wherein R ¹ , R ² , R ³ , X and / or Y are alkoxycarbonyl groups, or X or Y itself is alkoxy Carbonyl group) is hydrolyzed in a conventional manner, and if necessary, the carboxyl group of the compound in which X and Y are carboxyl groups is removed. The method according to claim 4, wherein the decarboxylation reaction is carried out in an acid medium. The method of claim 4 wherein the reaction is carried out at a temperature of 10 ° C. to 15 ° C. 6. A pharmaceutical product containing at least one or more of the compounds of the general formula (I) according to claim 1-3. A compound of formula (I) according to paragraphs 1-3, for the treatment of thromboembolism and anemia. Use for disease treatment of the compound of formula (I) according to paragraphs 1-3. A method for the preparation of a medicament according to claim 8, characterized in that the active compound or compounds are converted into a suitable dosage form using conventional adjuvants and / or excipients as necessary. ※ Note: The disclosure is based on the initial application.