HUP0302764A2 - Javított eljárás karbapenemszármazékok szintézisére - Google Patents

Javított eljárás karbapenemszármazékok szintézisére

Info

Publication number
HUP0302764A2
HUP0302764A2 HU0302764A HUP0302764A HUP0302764A2 HU P0302764 A2 HUP0302764 A2 HU P0302764A2 HU 0302764 A HU0302764 A HU 0302764A HU P0302764 A HUP0302764 A HU P0302764A HU P0302764 A2 HUP0302764 A2 HU P0302764A2
Authority
HU
Hungary
Prior art keywords
general formula
protecting group
formula
hydrogen atom
pharmaceutically acceptable
Prior art date
Application number
HU0302764A
Other languages
English (en)
Inventor
Renato T. Skerlj
John M. Williams
Original Assignee
Merck & 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 & Co., Inc. filed Critical Merck & Co., Inc.
Publication of HUP0302764A2 publication Critical patent/HUP0302764A2/hu
Publication of HUP0302764A3 publication Critical patent/HUP0302764A3/hu

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D477/00Heterocyclic 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
    • C07D477/10Heterocyclic 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
    • C07D477/12Heterocyclic 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
    • C07D477/16Heterocyclic 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
    • C07D477/20Sulfur atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D477/00Heterocyclic 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
    • C07D477/02Preparation
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

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

Abstract

A találmány tárgya egy fémkatalizátorból leszármaztatható fémetgyógyászatilag elfogadható mennyiségben tartalmazó (I) általánosképletű vegyületek - a képletben R1 és R2 egymástól függetlenülhidrogénatomot vagy adott esetben szubsztituált 1-10 szénatomottartalmazó alkilcsoportot vagy adott esetben szubsztituált, aril- vagyheteroarilcsoportot jelentenek - és gyógyászatilag elfogadható sóikelőállítására, azzal jellemezve, hogy egy (II) általános képletűvegyületet - a képletben R1 és R2 jelentése a tárgyi körben megadott,P jelentése karboxi-védőcsoport és P* jelentése hidrogénatom, H2<ionvagy hidrogenolízis útján eltávolítható védőcsoport - védőcsoportlehasítására szolgáló műveletnek vetnek alá egy előredukáltfémkatalizátor és egy bázis jelenlétében végrehajtott hidrogenolízisútján, majd a kapott (I) általános képletű vegyületet tisztítják éselkülönítik, továbbá kívánt esetben gyógyászatilag elfogadható sóváalakítják. Ó
HU0302764A 2001-01-16 2002-01-11 Improved process for carbapenem synthesis HUP0302764A3 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US26193301P 2001-01-16 2001-01-16
US29344001P 2001-05-24 2001-05-24
PCT/US2002/000821 WO2002057266A1 (en) 2001-01-16 2002-01-11 Improved process for carbapenem synthesis

Publications (2)

Publication Number Publication Date
HUP0302764A2 true HUP0302764A2 (hu) 2003-11-28
HUP0302764A3 HUP0302764A3 (en) 2005-11-28

Family

ID=26948925

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0302764A HUP0302764A3 (en) 2001-01-16 2002-01-11 Improved process for carbapenem synthesis

Country Status (29)

Country Link
US (1) US7071330B2 (hu)
EP (1) EP1353923B1 (hu)
JP (1) JP4098626B2 (hu)
KR (1) KR100827562B1 (hu)
CN (1) CN1249065C (hu)
AR (1) AR035728A1 (hu)
AT (1) ATE278691T1 (hu)
AU (1) AU2002234240B2 (hu)
BR (1) BR0206372A (hu)
CA (1) CA2433874C (hu)
CZ (1) CZ301440B6 (hu)
DE (1) DE60201498T2 (hu)
DK (1) DK1353923T3 (hu)
EA (1) EA006098B1 (hu)
EG (1) EG23993A (hu)
ES (1) ES2227423T3 (hu)
HR (1) HRP20030566B1 (hu)
HU (1) HUP0302764A3 (hu)
IL (2) IL156507A0 (hu)
MX (1) MXPA03006322A (hu)
NZ (1) NZ527191A (hu)
PL (1) PL362912A1 (hu)
PT (1) PT1353923E (hu)
RS (1) RS50494B (hu)
SI (1) SI1353923T1 (hu)
SK (1) SK287350B6 (hu)
TW (1) TWI318627B (hu)
UA (1) UA74870C2 (hu)
WO (1) WO2002057266A1 (hu)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1426376A4 (en) * 2001-08-13 2004-12-22 Eisai Co Ltd PROCESS FOR THE PREPARATION OF CARBAPENEM-BASED ANTIBIOTICS
CA2457642C (en) * 2001-09-26 2009-01-06 Merck & Co., Inc. Crystalline forms of ertapenem sodium
DK1474426T3 (da) * 2001-09-26 2011-11-21 Merck Sharp & Dohme Fremgangsmåde til fremstilling af carbapenemforbindelser
BR0214209A (pt) * 2001-11-16 2004-10-26 Ranbaxy Lab Ltd Processo para a preparação de imipenem cristalino e composto preparado pelo dito processo
JP4481829B2 (ja) * 2002-11-13 2010-06-16 株式会社カネカ 経口投与用カルバペネム化合物の新規合成中間体及びその製造方法
DE102005025899A1 (de) * 2005-06-06 2006-12-07 Basf Ag Verfahren zur Aufbereitung eines Alkoxycarbonylaminotriazin enthaltenden Reaktionsgemisches
AU2006290416B2 (en) * 2005-09-15 2012-04-12 Orchid Chemicals And Pharmaceuticals Limited An improved process for the preparation of beta-lactam antibiotic
JP5373390B2 (ja) * 2006-03-28 2013-12-18 株式会社カネカ カルバペネム化合物の改良された製造方法
US8293894B2 (en) 2006-11-20 2012-10-23 Orchid Chemicals & Pharmaceuticals Limited Process for the preparation of carbapenem antibiotic
CN101357920B (zh) * 2007-06-22 2011-01-12 山东轩竹医药科技有限公司 含有巯基吡咯烷甲酰胺基三嗪的培南化合物
CN101367807B (zh) * 2007-06-28 2011-01-12 山东轩竹医药科技有限公司 被巯基吡咯烷甲酰胺基吡啶取代的培南衍生物
JP2012525339A (ja) 2009-04-30 2012-10-22 石葯集団中奇制葯技▲術▼(石家庄)有限公司 エルタペネムの中間体、エルタペネムを含む組成物およびそれらの調製方法
CN102918041A (zh) * 2010-05-21 2013-02-06 山东轩竹医药科技有限公司 碳青霉烯衍生物或其水合物的晶型及其制备方法与用途
US8822445B2 (en) 2010-06-03 2014-09-02 Xuanzhu Pharma Co., Ltd. Crystalline form of carbapenem derivative or its hydrates and preparation methods and uses thereof
WO2012038979A2 (en) * 2010-09-24 2012-03-29 Sequent Anti Biotics Private Limited A process for preparation of ertapenem
CN102558182B (zh) 2010-12-31 2015-02-11 石药集团中奇制药技术(石家庄)有限公司 一种厄他培南钠晶型及其制备方法
WO2013121279A2 (en) * 2012-02-14 2013-08-22 Aurobindo Pharma Limited Process to prepare ertapenem
WO2014097221A1 (en) * 2012-12-21 2014-06-26 Ranbaxy Laboratories Limited Process for the purification of biapenem
US10011603B2 (en) * 2014-03-27 2018-07-03 Johnson Matthey Public Limited Company Process for preparing a carbapenem antibiotic

Family Cites Families (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BE794554A (fr) * 1972-01-31 1973-07-26 Lilly Co Eli Nouveaux derives de penicilline et de cephalusporine
US3925372A (en) * 1973-02-23 1975-12-09 Lilly Co Eli Alpha-aminoacyl-3-halo cephalosporins
US3897424A (en) * 1973-07-23 1975-07-29 Lilly Co Eli Process for 7-{62 -amino-7-{60 -methoxy-cephalosporanic acid esters and related compounds
AR207327A1 (es) * 1974-02-06 1976-09-30 Lilly Co Eli Un procedimiento para preparar acidos 3-cefem 3-sulfonatos y sus esteres
US4001226A (en) * 1974-12-04 1977-01-04 Eli Lilly And Company 3-(substituted)carbonylamino cephem derivatives
US3992377A (en) * 1974-12-13 1976-11-16 Eli Lilly And Company 3-Thio-substituted cephalosporin antibiotics
US3985746A (en) * 1975-03-25 1976-10-12 E. R. Squibb & Sons, Inc. 7-(α-Cyanomethylthio)acetamido-3-cephem carboxylates
US4217453A (en) * 1978-07-24 1980-08-12 Merck & Co., Inc. 6-Amido-3-substituted-amino-1-azabicyclo[3.2.0]hept-2-en-7-one-2-carboxylic acid
US4656263A (en) * 1979-03-05 1987-04-07 Pfizer Inc. 6-β-substituted penicillanic acid compound free of the 6-α-epimer
US4299954A (en) * 1979-11-05 1981-11-10 Eli Lilly And Company Cephalosporin vinyl halides
US4414155A (en) 1980-01-14 1983-11-08 Merck & Co., Inc. Synthesis of thienamycin via esters of (3SR, 4RS)-3-[(SR)-1-hydroxyethyl]-β,2-dioxo-4-azetidinebutanoic acid
US4269772A (en) 1980-01-14 1981-05-26 Merck & Co., Inc. Synthesis of thienamycin via trans-3-carboxymethylene-4-carboxy-5-methyl-Δ2 -isoxazoline
US4369187A (en) * 1980-02-06 1983-01-18 Merck & Co., Inc. 3-Substituted-1-azabicyclo[3.2.0]hept-2-en-7-one-2-carboxylic acid
US4383946A (en) 1980-03-27 1983-05-17 Merck & Co., Inc. Process for the preparation of 1-carbapenems and intermediates via silyl-substituted dithioacetals
US4501741A (en) * 1983-04-12 1985-02-26 Eli Lilly And Company Cephalosporin antibiotics
US4783453A (en) * 1985-06-10 1988-11-08 Merck & Co., Inc. 2-aza-substituted 1-carbadethiapen-2-em-3-carboxylic acids
JPS6475488A (en) * 1987-09-17 1989-03-22 Sumitomo Pharma Production of beta-lactam compound
US5034384A (en) 1990-08-01 1991-07-23 Merck & Co., Inc. 2-(9-fluorenonyl)-carbapenem antibacterial agents
GB9202298D0 (en) 1992-02-04 1992-03-18 Ici Plc Antibiotic compounds
CA2091309A1 (en) * 1992-03-26 1993-09-27 Frederic H. Jung Antibiotic compounds
HRP970281B1 (en) 1996-05-28 2002-04-30 Merck & Co Inc Carbapenem antibiotic, composition and method of preparation
UA62920C2 (en) 1996-05-28 2004-01-15 Merck & Co Inc Carbapeneme antibiotic, a composition and a method for the preparation
US6180783B1 (en) 1997-06-16 2001-01-30 Merck & Co., Inc. Stabilized carbapenem intermediates and improved process for carbapenem synthesis
US6063931A (en) 1997-07-09 2000-05-16 Merck & Co., Inc. Process for synthesizing carbapenem side chain intermediates
US5872250A (en) 1997-07-30 1999-02-16 Merck & Co., Inc. Process for synthesizing carbapenem antibiotics
AU749234B2 (en) * 1998-03-02 2002-06-20 Merck Sharp & Dohme Corp. Process for synthesizing carbapenem antibiotics

Also Published As

Publication number Publication date
MXPA03006322A (es) 2003-10-06
NZ527191A (en) 2004-04-30
BR0206372A (pt) 2003-12-23
AU2002234240B2 (en) 2006-04-27
EP1353923A1 (en) 2003-10-22
PL362912A1 (en) 2004-11-02
WO2002057266A1 (en) 2002-07-25
US20040063931A1 (en) 2004-04-01
RS50494B (sr) 2010-03-02
EP1353923B1 (en) 2004-10-06
CA2433874A1 (en) 2002-07-25
CZ301440B6 (cs) 2010-03-03
HRP20030566A2 (en) 2005-06-30
PT1353923E (pt) 2005-01-31
ATE278691T1 (de) 2004-10-15
CN1249065C (zh) 2006-04-05
HRP20030566B1 (en) 2011-08-31
EA200300804A1 (ru) 2003-12-25
ES2227423T3 (es) 2005-04-01
YU55003A (sh) 2006-05-25
CZ20031911A3 (cs) 2003-10-15
IL156507A0 (en) 2004-01-04
KR20040007438A (ko) 2004-01-24
SK8972003A3 (en) 2003-10-07
CN1486318A (zh) 2004-03-31
DE60201498T2 (de) 2005-11-17
DE60201498D1 (de) 2004-11-11
KR100827562B1 (ko) 2008-05-07
TWI318627B (en) 2009-12-21
JP2004518672A (ja) 2004-06-24
UA74870C2 (en) 2006-02-15
SI1353923T1 (en) 2005-02-28
JP4098626B2 (ja) 2008-06-11
HUP0302764A3 (en) 2005-11-28
EG23993A (en) 2008-03-10
CA2433874C (en) 2009-08-11
SK287350B6 (sk) 2010-08-09
AR035728A1 (es) 2004-07-07
US7071330B2 (en) 2006-07-04
IL156507A (en) 2010-06-30
DK1353923T3 (da) 2005-01-31
EA006098B1 (ru) 2005-08-25

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Legal Events

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GB9A Succession in title

Owner name: MERCK SHARP & DOHME CORP., US

Free format text: FORMER OWNER(S): MERCK & CO., INC., US

GB9A Succession in title

Owner name: MERCK SHARP & DOHME CORP., US

Free format text: FORMER OWNER(S): MERCK & CO., INC., US; MERCK SHARP & DOHME CORP., US; SCHERING CORPORATION, US

HC9A Change of name, address

Owner name: MERCK SHARP & DOHME CORP., US

Free format text: FORMER OWNER(S): MERCK & CO., INC., US; MERCK SHARP & DOHME CORP., US; SCHERING CORPORATION, US

FD9A Lapse of provisional protection due to non-payment of fees