ES8404184A1 - Un procedimiento para la prepracion de nuevos derivados de acidos 2-carbamimidoil-1-,carbadestiapen-2-en-3-carboxilados. - Google Patents

Un procedimiento para la prepracion de nuevos derivados de acidos 2-carbamimidoil-1-,carbadestiapen-2-en-3-carboxilados.

Info

Publication number
ES8404184A1
ES8404184A1 ES514240A ES514240A ES8404184A1 ES 8404184 A1 ES8404184 A1 ES 8404184A1 ES 514240 A ES514240 A ES 514240A ES 514240 A ES514240 A ES 514240A ES 8404184 A1 ES8404184 A1 ES 8404184A1
Authority
ES
Spain
Prior art keywords
carbamimidoyl
aryl
alkyl
hydrogen
inter alia
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
ES514240A
Other languages
English (en)
Other versions
ES514240A0 (es
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 ES8404184A1 publication Critical patent/ES8404184A1/es
Publication of ES514240A0 publication Critical patent/ES514240A0/es
Granted legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D477/00—Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring
    • C07D477/10—Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 4, and with a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 2
    • C07D477/12—Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 4, and with a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 2 with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached in position 6
    • C07D477/16—Heterocyclic compounds containing 1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbapenicillins, thienamycins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulphur-containing hetero ring with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 4, and with a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 2 with hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached in position 6 with hetero atoms or carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 3
    • C07D477/20—Sulfur atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C17/00—Preparation of halogenated hydrocarbons
    • C07C17/26—Preparation of halogenated hydrocarbons by reactions involving an increase in the number of carbon atoms in the skeleton
    • C07C17/272—Preparation of halogenated hydrocarbons by reactions involving an increase in the number of carbon atoms in the skeleton by addition reactions
    • C07C17/275—Preparation of halogenated hydrocarbons by reactions involving an increase in the number of carbon atoms in the skeleton by addition reactions of hydrocarbons and halogenated hydrocarbons
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/61—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups
    • C07C45/67—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton
    • C07C45/68—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms
    • C07C45/72—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms by reaction of compounds containing >C = O groups with the same or other compounds containing >C = O groups
    • C07C45/74—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms by reaction of compounds containing >C = O groups with the same or other compounds containing >C = O groups combined with dehydration
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C67/00—Preparation of carboxylic acid esters
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/06—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D205/08—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with one oxygen atom directly attached in position 2, e.g. beta-lactams
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/04—1,3-Oxazines; Hydrogenated 1,3-oxazines
    • C07D265/12—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems
    • C07D265/14—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/10—Compounds having one or more C—Si linkages containing nitrogen having a Si-N linkage
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804—Compounds having Si-O-C linkages

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Cephalosporin Compounds (AREA)

Abstract

PROCEDIMIENTO PARA LA OBTENCION DE DERIVADOS DE ACIDOS 2-CARBAMIDOIL-1-CARBADESTIAPEN-2-EM-3-CARBOXILI COS Y DE SUS SALES, ESTERES Y AMIDAS FISIOLOGICAMENTE COMPATIBLES, DE FORMULA (I), EN LA QUE R, R, R, R Y R PUEDEN SER VARIOS RADICALES.CONSISTE EN LA REACCION DE SUSTITUCION DE UN COMPUESTO DE FORMULA (II), CON UN EQUIVALENTE O MAS DE UN MERCAPTANO DE FORMULA HSR, EN LA QUE XA ES UN GRUPO SALIENTE, R ES UN GRUPO PROTECTOR Y LOS DEMAS SIMBOLOS TIENEN EL MISMO SIGNIFICADO QUE EN LA FORMULA (I), SEGUIDA DEL DESBLOQUEO DEL COMPUESTO OBTENIDO. LA REACCION SE EFECTUA EN UNDISOLVENTE APROTICO, EN PRESENCIA DE UNA BASE, A TEMPERATURAS ENTRE C40JC Y 25JC.ESTOS COMPUESTOS TIENEN APLICACIONES FARMACOLOGICAS POR SU EFECTO ANTIBIOTICO.
ES514240A 1981-08-03 1982-07-22 Un procedimiento para la prepracion de nuevos derivados de acidos 2-carbamimidoil-1-,carbadestiapen-2-en-3-carboxilados. Granted ES514240A0 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US28959981A 1981-08-03 1981-08-03
US28934581A 1981-08-03 1981-08-03
US28960081A 1981-08-03 1981-08-03

Publications (2)

Publication Number Publication Date
ES8404184A1 true ES8404184A1 (es) 1984-04-16
ES514240A0 ES514240A0 (es) 1984-04-16

Family

ID=27403880

Family Applications (1)

Application Number Title Priority Date Filing Date
ES514240A Granted ES514240A0 (es) 1981-08-03 1982-07-22 Un procedimiento para la prepracion de nuevos derivados de acidos 2-carbamimidoil-1-,carbadestiapen-2-en-3-carboxilados.

Country Status (10)

Country Link
EP (1) EP0071908B1 (es)
JP (1) JPS5826887A (es)
AT (1) ATE46696T1 (es)
CA (1) CA1198427A (es)
DE (1) DE3279960D1 (es)
DK (1) DK344882A (es)
ES (1) ES514240A0 (es)
GR (1) GR76873B (es)
IE (1) IE55401B1 (es)
PT (1) PT75357B (es)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4683301A (en) * 1982-04-08 1987-07-28 Bristol-Myers Company Carbapenem antibiotics
FI832619A (fi) * 1982-07-26 1984-01-27 Sandoz Ag Fluoralkylerade karbapenemderivat
ZA836966B (en) * 1982-09-28 1984-04-25 Bristol Myers Co Carbapenem antibiotics
US4732977A (en) * 1982-09-28 1988-03-22 Bristol Myers Company Carbapenem antibiotics
US4746736A (en) * 1982-09-28 1988-05-24 Bristol-Myers Company Carbapenem antibiotics
CA1283906C (en) * 1983-05-09 1991-05-07 Makoto Sunagawa .beta.-LACTAM COMPOUNDS AND PRODUCTION THEREOF
CH662117A5 (de) * 1983-10-03 1987-09-15 Sanraku Inc Carbapenemderivate und verfahren zu ihrer herstellung.
US4748238A (en) * 1984-03-14 1988-05-31 Merck & Co., Inc. Crystalline 1R,5S,6S,8R-1-methyl-2-(N,N-dimethylcarbamimidoylmethylthio)-6-(1-hydroxyethyl)-1-carbapen-2-em-3-carboxylic acid
JPS60202886A (ja) * 1984-03-27 1985-10-14 Sankyo Co Ltd １―置換カルバペネム―３―カルボン酸誘導体
US4696923A (en) * 1984-04-23 1987-09-29 Merck & Co., Inc. 6-[1-hydroxyethyl]-2-SR8 -1-methyl-1-carbadethiapen-2-em-3-carboxylic acids
DE3581481D1 (de) * 1984-10-31 1991-02-28 Sumitomo Pharma Beta-lactame und ihre herstellung.
CA1281720C (en) * 1984-11-08 1991-03-19 Makoto Sunagawa Carbapenem compounds and production thereof
US5310897A (en) * 1984-12-27 1994-05-10 Sumitomo Pharmaceuticals Co., Ltd. Beta-lactams and their production
US5104984A (en) * 1985-03-29 1992-04-14 Merck & Co., Inc. Enantioselective process for producing 1-beta-methyl carbapenem antibiotic intermediates
ES8800215A1 (es) * 1985-03-29 1987-10-16 Merck & Co Inc Un procedimiento enantioselectivo para la preparacion de intermedios para los antibioticos de 1-b-metil-carbapenem
DK189686A (da) * 1985-04-27 1986-10-28 Sankyo Co Carbapenemforbindelser og fremgangsmaade til fremstilling deraf samt middel indeholdende forbindelserne
JPS62103063A (ja) * 1985-10-29 1987-05-13 Sagami Chem Res Center アゼチジノン誘導体の製造方法
EP0229384B1 (en) * 1985-12-28 1994-08-10 Sumitomo Pharmaceuticals Company, Limited Beta-lactam compounds and their production
JPH0759581B2 (ja) * 1986-09-05 1995-06-28 日本レダリ−株式会社 （１ｒ）−１−メチルカルバペネム−３−カルボン酸誘導体
JPS6363680A (ja) * 1986-09-05 1988-03-22 Nippon Redarii Kk （１ｒ）−１−メチルカルバペネム−３−カルボン酸誘導体
JPH0713058B2 (ja) * 1986-12-29 1995-02-15 日本レダリ−株式会社 ４―置換アゼチジノン誘導体の製造方法
DE68916908T2 (de) * 1988-11-08 1994-12-01 Daiichi Seiyaku Co Carbapenemderivate.
US5672701A (en) * 1990-01-16 1997-09-30 Bristol-Myers Squibb Company 4-substituted alkyl carbapenem antibiotics
EP0546742B1 (en) * 1991-12-09 2001-06-20 Takasago International Corporation 4-(1,1-Dialkoxycarbonyl-alkyl)azetidin-2-one derivatives and synthesis of 4-(1-carboxy-alkyl)azetidin-2-one derivatives therefrom
US5750686A (en) * 1993-06-16 1998-05-12 Sumitomo Pharmaceuticals Company, Limited Carbapenem compounds and process for producing the same
US5496816A (en) * 1994-03-14 1996-03-05 Merck & Co., Inc. Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment
JPH1077285A (ja) 1996-09-04 1998-03-24 Sumitomo Pharmaceut Co Ltd 新規なβ−ラクタム化合物およびその製造法
US20020049315A1 (en) * 2000-09-06 2002-04-25 Williams John M. Crystalline forms of carbapenem intermediates

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IE51861B1 (en) * 1978-10-24 1987-04-15 Merck & Co Inc 6-,1-and 2-substituted-1-carbapen-2-em-3-carboxylic acids,processes for the preparation of such compounds and pharmaceutical compositions comprising such compounds
US4260627A (en) * 1978-10-24 1981-04-07 Merck & Co., Inc. 1-, 6- And 2-substituted-1-carba-2-penem-3-carboxylic acids
EP0017992A1 (en) * 1979-04-19 1980-10-29 Merck & Co. Inc. 2-Substituted-6-substituted-1-carbadethiapen-2-em-3-carboxylic acids, processes for preparing them, antibiotic pharmaceutical compositions containing same and process for preparing intermediates
GR72296B (es) * 1979-12-03 1983-10-18 Merck & Co Inc
EP0038869A1 (en) * 1980-04-30 1981-11-04 Merck & Co. Inc. Process for the preparation of 1-carbapenems, and intermediates for their preparation
PT73791B (en) * 1980-10-17 1983-10-14 Merck & Co Inc Process for preparing 2-carbamimidoyl-6-substituted-1- -carbadethiapen-2-em-3-carboxylic acids
EP0060077A1 (en) * 1981-03-04 1982-09-15 Beecham Group Plc Beta-lactam antibiotics, their preparation and use

Also Published As

Publication number Publication date
EP0071908A1 (en) 1983-02-16
IE821846L (en) 1983-02-03
DK344882A (da) 1983-02-04
ATE46696T1 (de) 1989-10-15
JPS5826887A (ja) 1983-02-17
PT75357B (en) 1985-11-20
IE55401B1 (en) 1990-09-12
DE3279960D1 (en) 1989-11-02
ES514240A0 (es) 1984-04-16
GR76873B (es) 1984-09-04
EP0071908B1 (en) 1989-09-27
PT75357A (en) 1982-09-01
JPH0545596B2 (es) 1993-07-09
CA1198427A (en) 1985-12-24

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FD1A Patent lapsed

Effective date: 19991108