ATE141265T1 - Verfahren zur herstellung von intermediaten in der synthese von retroviralen protease inhibitoren - Google Patents

Verfahren zur herstellung von intermediaten in der synthese von retroviralen protease inhibitoren

Info

Publication number
ATE141265T1
ATE141265T1 AT93911369T AT93911369T ATE141265T1 AT E141265 T1 ATE141265 T1 AT E141265T1 AT 93911369 T AT93911369 T AT 93911369T AT 93911369 T AT93911369 T AT 93911369T AT E141265 T1 ATE141265 T1 AT E141265T1
Authority
AT
Austria
Prior art keywords
substituted
alkyl
arylalkyl
synthesis
protease inhibitors
Prior art date
Application number
AT93911369T
Other languages
English (en)
Inventor
John S Ng
Claire A Przybyla
Richard A Mueller
Michael L Vazquez
Daniel P Getman
Original Assignee
Searle & Co
Monsanto Co
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 Searle & Co, Monsanto Co filed Critical Searle & Co
Application granted granted Critical
Publication of ATE141265T1 publication Critical patent/ATE141265T1/de

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0207—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)4-C(=0), e.g. 'isosters', replacing two amino acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C213/00—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C213/00—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
    • C07C213/02—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions involving the formation of amino groups from compounds containing hydroxy groups or etherified or esterified hydroxy groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C213/00—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
    • C07C213/08—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions not involving the formation of amino groups, hydroxy groups or etherified or esterified hydroxy groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/04—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms
    • C07C275/20—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an unsaturated carbon skeleton
    • C07C275/22—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing rings other than six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/04—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms
    • C07C275/20—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an unsaturated carbon skeleton
    • C07C275/24—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/44—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D303/00—Compounds containing three-membered rings having one oxygen atom as the only ring hetero atom
    • C07D303/02—Compounds containing oxirane rings
    • C07D303/36—Compounds containing oxirane rings with hydrocarbon radicals, substituted by nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers
    • Y—GENERAL 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
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Molecular Biology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Medicinal Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Epoxy Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AT93911369T 1992-05-20 1993-05-20 Verfahren zur herstellung von intermediaten in der synthese von retroviralen protease inhibitoren ATE141265T1 (de)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US88655892A 1992-05-20 1992-05-20

Publications (1)

Publication Number Publication Date
ATE141265T1 true ATE141265T1 (de) 1996-08-15

Family

ID=25389250

Family Applications (1)

Application Number Title Priority Date Filing Date
AT93911369T ATE141265T1 (de) 1992-05-20 1993-05-20 Verfahren zur herstellung von intermediaten in der synthese von retroviralen protease inhibitoren

Country Status (11)

Country Link
EP (1) EP0641333B1 (de)
JP (3) JP3492362B2 (de)
KR (1) KR100290516B1 (de)
AT (1) ATE141265T1 (de)
AU (2) AU4253193A (de)
CA (1) CA2131182C (de)
DE (1) DE69304051T2 (de)
DK (1) DK0641333T3 (de)
ES (1) ES2091000T3 (de)
GR (1) GR3020814T3 (de)
WO (2) WO1993023368A1 (de)

Families Citing this family (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6878728B1 (en) 1999-06-11 2005-04-12 Vertex Pharmaceutical Incorporated Inhibitors of aspartyl protease
US20040122000A1 (en) 1981-01-07 2004-06-24 Vertex Pharmaceuticals Incorporated. Inhibitors of aspartyl protease
DK0810209T3 (da) 1992-08-25 2002-08-12 Monsanto Co Alpha - and beta-aminosyre-hydroxyethylaminosulfonamider til anvendelse som inhibitorer af retrovirale proteaser
US7141609B2 (en) 1992-08-25 2006-11-28 G.D. Searle & Co. α- and β-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors
IS2334B (is) * 1992-09-08 2008-02-15 Vertex Pharmaceuticals Inc., (A Massachusetts Corporation) Aspartyl próteasi hemjari af nýjum flokki súlfonamíða
US5783701A (en) 1992-09-08 1998-07-21 Vertex Pharmaceuticals, Incorporated Sulfonamide inhibitors of aspartyl protease
US5723490A (en) * 1992-09-08 1998-03-03 Vertex Pharmaceuticals Incorporated THF-containing sulfonamide inhibitors of aspartyl protease
US6046175A (en) * 1993-05-21 2000-04-04 The United States Of America As Represented By The Department Of Health And Human Services Procedure to block the replication of reverse transcriptase dependent viruses by the use of inhibitors of deoxynucleotides synthesis
AU7518694A (en) * 1993-08-20 1995-03-21 G.D. Searle & Co. Retroviral protease inhibitors and combinations thereof
US6093702A (en) * 1993-12-20 2000-07-25 The United States Of America As Represented By The Department Of Health And Human Services Mixtures of dideoxy-nucleosides and hydroxycarbamide for inhibiting retroviral spread
DE69512220T2 (de) * 1994-03-07 2000-03-16 Vertex Pharmaceuticals Inc. Sulfonamidderivate als aspartylprotease-inhibitoren
US5475138A (en) * 1994-07-07 1995-12-12 Pharm-Eco Laboratories Incorporated Method preparing amino acid-derived diaminopropanols
CA2137406C (en) * 1994-12-06 2005-09-13 Pierre Louis Beaulieu Process for key intermediates for hiv protease inhibitors
US5481011A (en) * 1994-12-13 1996-01-02 Bristol-Myers Squibb Company Process for preparing N-protected amino acid α-halomethyl ketones and alcohols from N-protected amino acid esters
EP0804428B1 (de) * 1995-01-20 2007-12-26 G.D. Searle LLC. Bis-sulfonamid-hydroxyethylamino-derivate als inhibitoren retroviraler proteasen
US5831117A (en) 1995-01-20 1998-11-03 G. D. Searle & Co. Method of preparing retroviral protease inhibitor intermediates
US5693847A (en) * 1995-04-19 1997-12-02 Vertex Pharmaceuticals Incorporated Heteroatom functionalized α-methyl ketones
US5691372A (en) * 1995-04-19 1997-11-25 Vertex Pharmaceuticals Incorporated Oxygenated-Heterocycle containing sulfonamide inhibitors of aspartyl protease
US6004957A (en) * 1995-06-07 1999-12-21 Vertex Pharmaceuticals, Incorporated Sulfonamide inhibitors of aspartyl protease
US6037157A (en) 1995-06-29 2000-03-14 Abbott Laboratories Method for improving pharmacokinetics
US6063963A (en) * 1995-07-05 2000-05-16 Pharm-Eco Laboratories, Inc. Amino acid-derived diaminopropanols
CA2237936A1 (en) * 1995-11-16 1997-05-22 G.D. Searle & Co. N-protected/n-substituted-beta-amino hydroxy sulfonates
CA2190570C (en) 1995-11-17 2005-05-03 Yutaka Honda Process for producing 3-amino-2-oxo-1-halogenopropane derivatives
US5914332A (en) 1995-12-13 1999-06-22 Abbott Laboratories Retroviral protease inhibiting compounds
US5919956A (en) * 1996-10-18 1999-07-06 Roche Vitamins Inc. Process for the C1 -homologization of protected phorenol
US6232333B1 (en) 1996-11-21 2001-05-15 Abbott Laboratories Pharmaceutical composition
ZA9710071B (en) * 1996-11-21 1998-05-25 Abbott Lab Pharmaceutical composition.
US6127556A (en) * 1996-12-31 2000-10-03 G. D. Searle & Co. Epoxide formation by continuous in-situ synthesis process
US6436989B1 (en) 1997-12-24 2002-08-20 Vertex Pharmaceuticals, Incorporated Prodrugs of aspartyl protease inhibitors
AU767728B2 (en) 1998-06-19 2003-11-20 Vertex Pharmaceuticals Incorporated Sulfonamide inhibitors of aspartyl protease
BR0011864A (pt) 2000-01-19 2004-07-20 Abbott Lab Formulações farmacêuticas
FR2820136A1 (fr) * 2001-01-26 2002-08-02 Aventis Pharma Sa Nouveaux derives de l'uree, leur procede de preparation, leur application a titre de medicaments, compositions pharmaceutiques et nouvelle utilisation
FR2885129B1 (fr) 2005-04-29 2007-06-15 Proskelia Sas Nouveaux derives de l'ureee substituee parun thiazole ou benzothiazole, leur procede de preparation, leur application a titre de medicaments, les compositions pharmaceutiques les renfermant et utilisation.
AU2006316705B2 (en) 2005-11-25 2011-09-29 Galapagos Sas Urea derivatives useful as calcium receptor modulators
WO2008112289A2 (en) 2007-03-12 2008-09-18 Nektar Therapeutics Oligomer-protease inhibitor conjugates
WO2009114151A1 (en) 2008-03-12 2009-09-17 Nektar Therapeutics Oligomer-amino acid and olgomer-atazanavir conjugates
JP2012530069A (ja) 2009-06-12 2012-11-29 ネクター セラピューティックス プロテアーゼ阻害剤、水溶性非ペプチドオリゴマーおよび親油性部分を含む共有結合体
CN112546969B (zh) * 2020-12-07 2022-12-23 安徽贝克制药股份有限公司 催化加氢连续生产装置和利托那韦中间体的制备方法

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA1297631C (en) * 1985-12-23 1992-03-17 Sesha I. Natarajan Ureido renin inhibitors
DE3635907A1 (de) * 1986-10-22 1988-04-28 Merck Patent Gmbh Hydroxy-aminosaeurederivate
GB2200115B (en) * 1987-01-21 1990-11-14 Sandoz Ltd Novel peptide derivatives, their production and use
USH725H (en) * 1987-02-26 1990-01-02 E. R. Squibb & Sons, Inc. Ureido amino and imino acids, compositions and methods for use
DE3711911A1 (de) * 1987-04-08 1988-10-20 Bayer Ag Optisch aktive (alpha)-aminoaldehyde, verfahren zu ihrer herstellung und ihre verwendung zur stereoselektiven herstellung optisch aktiver ss-aminoalkohole
EP0374097A3 (de) * 1988-12-15 1991-06-12 Ciba-Geigy Ag Verwendung von Peptidisosteren als retrovirale Proteasehemmer
ES2243959T3 (es) * 1990-11-19 2005-12-01 Monsanto Company Inhibidores de proteasas retrovirales.

Also Published As

Publication number Publication date
EP0641333B1 (de) 1996-08-14
GR3020814T3 (en) 1996-11-30
WO1993023388A1 (en) 1993-11-25
AU4253193A (en) 1993-12-13
WO1993023368A1 (en) 1993-11-25
JP2003160545A (ja) 2003-06-03
JPH07508041A (ja) 1995-09-07
ES2091000T3 (es) 1996-10-16
DK0641333T3 (da) 1996-09-02
AU4253093A (en) 1993-12-13
DE69304051D1 (de) 1996-09-19
EP0641333A1 (de) 1995-03-08
DE69304051T2 (de) 1997-01-23
KR100290516B1 (ko) 2001-09-17
JP3492362B2 (ja) 2004-02-03
AU676479B2 (en) 1997-03-13
CA2131182A1 (en) 1993-11-25
CA2131182C (en) 2005-04-26
JP2003192648A (ja) 2003-07-09
KR950700893A (ko) 1995-02-20

Similar Documents

Publication Publication Date Title
DE69304051D1 (de) Verfahren zur herstellung von intermediaten in der synthese von retroviralen protease inhibitoren
DE59108707D1 (de) Verfahren zur Herstellung von Oxetanonen
DK89595A (da) Fremgangsmåde til fremstilling af 1-(3-dimethylaminopropyl)-1'-(4-fluorphenyl)-1,3-dihydroisobenzofuran-5-carbonnitril
DE69719201D1 (de) Verfahren zur herstellung von ecteinascidin-verbindungen
ATE264268T1 (de) Verfahren zur herstellung von zsm-5 und zsm-11
ATE26263T1 (de) 1-aryloxy-2,3,4,5-tetrahydro-3-benzazepine, verfahren zur herstellung derselben und ihre verwendung als heilmittel.
DE69325031D1 (de) Verfahren zur herstellung von taxanderivaten
ATE210136T1 (de) Verfahren zur herstellung von alkylhydrogenchlorsilanen
DE3576952D1 (de) Verfahren zur herstellung von 4-phenyl-pyrrol-derivaten.
DE69524578D1 (de) Verfahren zur herstellung von epoxiden
ATE380173T1 (de) Verfahren zur herstellung von (2s,3r,4s)-4- hydroxyisoleucin und analoga
ATE372332T1 (de) Verfahren zur herstellung von zwischenverbindungen in der herstellung von discodermolid und discodermolid-analoga
ATE179972T1 (de) Pyridazinone-derivate und verfahren zur deren herstellung
DE69531219D1 (de) Verfahren zur umwandlung von 2,4-dichlorpyridinen in 2-aryloxy-4-chlorpyridine
DE69619230D1 (de) Oxidatives verfahren zur herstellung von narwedin-derivaten
DE69839732D1 (de) Verfahren zur herstellung von 3,4-dihydroxy-3cyclobuten-1,2-dion
DE69411783D1 (de) Verfahren zur Herstellung von Sulfonylharnstoffderivaten
DE69714749D1 (de) Verfahren zur herstellung von 3-amino-2-hydroxy-1-propylethern
ATE63107T1 (de) Verfahren zur synthese von carbonsaeuren.
DE68902673D1 (de) Verfahren zur herstellung von oxalsaeureestern und -amiden.
ATE27955T1 (de) Verfahren und zwischenprodukte zur herstellung von 2-substituierten 4-acetyl-imidazolen.
DE59915198D1 (de) Verfahren zur herstellung von 1-substituierten 5-hydroxypyrazolen
ATE42299T1 (de) Verfahren zur herstellung von n(dibenzyloxyphosphoryl)-cyanamid und die verfahren, die solche verbindungen als zwischenprodukt fuer die synthese von phosphagenstoffen verwenden.
DE69916287D1 (de) Verfahren zur synthese von carbapenem-zwischenprodukten
ATE27281T1 (de) Verfahren zur herstellung von oxanosin.

Legal Events

Date Code Title Description
UEP Publication of translation of european patent specification
REN Ceased due to non-payment of the annual fee