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GB1049031A - Malonic acid derivatives - Google Patents

Malonic acid derivatives

Info

Publication number
GB1049031A
GB1049031A GB714764A GB714764A GB1049031A GB 1049031 A GB1049031 A GB 1049031A GB 714764 A GB714764 A GB 714764A GB 714764 A GB714764 A GB 714764A GB 1049031 A GB1049031 A GB 1049031A
Authority
GB
United Kingdom
Prior art keywords
acid
acids
diethyl
alkoxy
pyrone
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired
Application number
GB714764A
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck and Co Inc
Original Assignee
Merck and Co Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merck and Co Inc filed Critical Merck and Co Inc
Publication of GB1049031A publication Critical patent/GB1049031A/en
Expired legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/40Unsaturated compounds
    • C07C59/58Unsaturated compounds containing ether groups, groups, groups, or groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/79Acids; Esters
    • C07D213/80Acids; Esters in position 3
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D309/00Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/34Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D309/36Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with oxygen atoms directly attached to ring carbon atoms
    • C07D309/38Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with oxygen atoms directly attached to ring carbon atoms one oxygen atom in position 2 or 4, e.g. pyrones
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D499/00Heterocyclic compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. penicillins, penems; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Catalysts (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Abstract

The invention comprises allylidenemalonic acid compounds of formula <FORM:1049031/C2/1> where R and R1 represent hydrogen or alkyl radicals, R2 an alkoxy or -NHR4 where R4 represents hydrogen or an alkyl, aryl or aralkyl radical, specifically diethyl esters of 3(C1-C5) alkoxy allylidene malonic acids, 3-aminoallylidenemalonic acid, diethyl-3-amino-allylidencemalonate, 3-alkylaminoallylidene-malonic acids and their diethyl esters. The 3-alkoxy-allylidene-malonic acid compound is prepared by reacting in the presence of a Lewis acid a tetraalkoxypropane of formula <FORM:1049031/C2/2> with malonic acid or an alkyl ester thereof, and the 3-amino acids are prepared by a further reaction with ammonia, a primary alkylamine, arylamine or aralkylamine. The alkoxy acids may be cyclized by heating in the presence of a strong acid to produce a -pyrone-3-carboxylic acids, and the amino-acids may be cyclized with a base to yield a -pyridone-3-carboxylic acid. Examples describe the preparation of diethylethoxyallylidenemalonate, 3 - ethoxyallylidenemalonic acid, diethyl-3-aminoallylidenemalonate, diethyl - 3 - benzylaminoallylidene malonate, ethyl - a - pyrone - 3 - carboxylate, a - pyrone - 3 - carboxylic acid, ethyland ethyl - N - benzyl - a - pyridone - 3 - carbxylate and N - benzyl - a - pyridone - 3 - carboxylic acid. The alkoxyallylidene diethyl malonate may be reacted with urea in the presence of sodium methoxide to form 5-(alkoxy - aminoallylidene) barbituric acid and equal molar amounts of 6-aminopenicillanic acid and a -pyrone-3-carboxylic acid reacted in the presence of dicyclohexyl-carbodiimide forms a penicillin of formula <FORM:1049031/C2/3>
GB714764A 1963-03-06 1964-02-20 Malonic acid derivatives Expired GB1049031A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US26310963A 1963-03-06 1963-03-06

Publications (1)

Publication Number Publication Date
GB1049031A true GB1049031A (en) 1966-11-23

Family

ID=23000404

Family Applications (1)

Application Number Title Priority Date Filing Date
GB714764A Expired GB1049031A (en) 1963-03-06 1964-02-20 Malonic acid derivatives

Country Status (3)

Country Link
DE (1) DE1468312A1 (en)
GB (1) GB1049031A (en)
NL (1) NL6402325A (en)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1986001202A1 (en) * 1984-08-03 1986-02-27 American Hospital Supply Corporation Pyridone esters as inotropic agents
CN117658900A (en) * 2022-08-30 2024-03-08 南京药石科技股份有限公司 A kind of preparation method of tetrahydronaphthyridine compounds and its intermediates

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1986001202A1 (en) * 1984-08-03 1986-02-27 American Hospital Supply Corporation Pyridone esters as inotropic agents
CN117658900A (en) * 2022-08-30 2024-03-08 南京药石科技股份有限公司 A kind of preparation method of tetrahydronaphthyridine compounds and its intermediates
CN117658900B (en) * 2022-08-30 2025-11-21 南京药石科技股份有限公司 Preparation method of tetrahydronaphthyridine compound and intermediate thereof

Also Published As

Publication number Publication date
DE1468312A1 (en) 1968-11-28
NL6402325A (en) 1964-09-07

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