KR910015586A - Novel cephalosporin compounds and preparation methods thereof - Google Patents

Abstract

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Description

Novel cephalosporin compounds and preparation methods thereof

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Claims (13)

The cephalosporin compound represented by the following general formula (I) and its pharmaceutically acceptable non-toxic salts, physiologically hydrolysable esters, hydrates and solvates thereof. Wherein R ¹ is a C _1-4 alkyl group, C _3-4 alkenyl group, C _3-4 alkynyl group, or —C (R ^a ) (R ^b ) CO ₂ H, and R ¹ is —C (R ^a ) (R ^b) CO ₂ H when R ^a R ^b may be the same or different and each represent a C _1-4 alkyl group, or represents hydrogen or R ^a and R ^b is a C _3-7 cycloalkyl group together with the carbon atoms to which they are bonded And R ² is an alkyl group or an aryl group. The compound of claim 1, wherein the compound is 7-[(Z) -2- (2-aminothiazol-4-yl) -2- (2-carboxyprop-2-oxyimino) acetamido] -3- A cephalosporin compound that is (4,6-diamino-1-ethyl-1,3,5-triazinium-2-yl) thiomethyl-3-cepem-4-carboxylate and a pharmaceutically acceptable thereof Nontoxic salts, physiologically hydrolysable esters, hydrates and solvates thereof. The compound of claim 1, wherein the compound is 7-[(Z) -2- (2-aminothiazol-4-yl) -2- (2-carboxyprop-2-oxyimino) acetamido] -3- A cephalosporin compound that is (4,6-diamino-1-ethyl-1,3,5-triazinium-2-yl) thiomethyl-3-cepem-4-carboxylate and a pharmaceutically acceptable thereof Nontoxic salts, physiologically hydrolysable esters, hydrates and solvates thereof. The compound of claim 1, wherein the compound is 7-[(Z) -2- (2-aminothiazol-4-yl) -2- (2-carboxyprop-2-oxyimino) acetamido] -3- A cephalosporin compound that is (4,6-diamino-1-ethyl-1,3,5-triazinium-2-yl) thiomethyl-3-cepem-4-carboxylate and a pharmaceutically acceptable thereof Nontoxic salts, physiologically hydrolysable esters, hydrates and solvates thereof. The cephalosporin compound represented by the following general formula (I) and a pharmaceutically acceptable compound are reacted with a compound represented by the following general formula (III) in the presence of a solvent: Its non-toxic salts, physiologically hydrolysable esters, hydrates and solvates thereof. Wherein R ¹ is a C _1-4 alkyl group, C _3-4 alkynyl group, or —C (R ^a ) (R ^b ) CO ₂ H, and R ¹ is —C (R ^a ) (R ^b ) CO ₂ H R ^a R ^b may be the same or different and each represents hydrogen or a C _1-4 alkyl group or R ^a R ^b together with the carbon atom to which they are attached form a C _3-7 cycloalkyl group, and R ² is An alkyl group or an aryl group, R ³ is a C _1-4 alkyl group, C _3-4 alkenyl group, C _3-4 alkynyl group, or —C (R ^a ) (R ^b ) CO ₂ (R ^c ) group, wherein R ^a and R ^b may be the same or different and each may represent hydrogen or a C _1-4 alkyl group or R ^a and R ^b together with the carbon atom to which they are attached may form a C _3-7 cycloalkyl group, R ^c Is a hydrogen or a carboxyl protecting group, R ⁴ is a hydrogen or an amino code group, R ⁶ is a hydrogen or a carboxyl protecting group, L is a leaving group and n is 0 or 1. The method according to claim 5, wherein the solvent is water or a mixed aqueous solution of water and a water miscible solvent. The method of claim 5 wherein the water miscible solvent is acetonitrile or acetone. The method according to claim 5, wherein the amount of the compound of the general formula (III) is 1 to 2 equivalents based on the compound of the general formula (II). Wherein R ² , R ³ , R ⁴ , R ⁵ , R ⁶ , L and n are as defined above. 6. The method of claim 5 wherein the solvent is maintained at a pH of 5-8. The method of claim 5 wherein the reaction is carried out in the presence of a stabilizer. The method of claim 10, wherein the stabilizing agent is one or more selected from sodium iodide, potassium iodide, bromosodium, bromopotassium or potassium thiocyanate. The method according to claim 5, wherein the amino protecting group or acid protecting group is removed or the S-oxide is reduced before or after reacting the compound of formula (II) with the compound of formula (III). Wherein R ² , R ³ , R ⁴ , R ⁵ , R ⁶ , L and n are as defined above. A therapeutically effective compound of at least one of the cephalosporin compound according to any one of claims 1 to 6 and a pharmaceutically acceptable non-toxic salt thereof, physiologically hydrolysable ester, hydrate and solvate thereof as an active ingredient. A pharmaceutical composition comprising an amount and a pharmaceutically acceptable carrier, excipient or additive. ※ Note: The disclosure is based on the initial application.