WO1995002584A3 - Process for making hiv protease inhibitors - Google Patents

Process for making hiv protease inhibitors Download PDF

Info

Publication number
WO1995002584A3
WO1995002584A3 PCT/US1994/007706 US9407706W WO9502584A3 WO 1995002584 A3 WO1995002584 A3 WO 1995002584A3 US 9407706 W US9407706 W US 9407706W WO 9502584 A3 WO9502584 A3 WO 9502584A3
Authority
WO
WIPO (PCT)
Prior art keywords
hiv protease
protease inhibitors
making hiv
intermediates
making
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.)
Ceased
Application number
PCT/US1994/007706
Other languages
French (fr)
Other versions
WO1995002584A2 (en
Inventor
David Askin
Ralph P Volante
Kan K Eng
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
Priority claimed from US08/187,664 external-priority patent/US5463067A/en
Priority to SK55-96A priority Critical patent/SK282616B6/en
Priority to EP94922511A priority patent/EP0708762B1/en
Priority to DE69426979T priority patent/DE69426979T2/en
Priority to JP50463295A priority patent/JP3547136B2/en
Priority to AU73588/94A priority patent/AU676079B2/en
Priority to AT94922511T priority patent/ATE200079T1/en
Priority to DK94922511T priority patent/DK0708762T3/en
Priority to CA002167183A priority patent/CA2167183C/en
Application filed by Merck and Co Inc filed Critical Merck and Co Inc
Priority to RU96103642A priority patent/RU2125561C1/en
Priority to NZ269904A priority patent/NZ269904A/en
Priority to PL94312613A priority patent/PL179039B1/en
Priority to KR1019960700208A priority patent/KR100329694B1/en
Publication of WO1995002584A2 publication Critical patent/WO1995002584A2/en
Publication of WO1995002584A3 publication Critical patent/WO1995002584A3/en
Priority to FI960184A priority patent/FI119473B/en
Priority to NO960168A priority patent/NO306297B1/en
Anticipated expiration legal-status Critical
Priority to GR20010400119T priority patent/GR3035645T3/en
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Epoxy Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Intermediates of structural formula (IV) can be made by reacting glycidol or an activated derivative thereof with an amide. The process and intermediates are useful for synthesizing HIV protease inhibitor compounds.
PCT/US1994/007706 1993-07-16 1994-07-11 Process for making hiv protease inhibitors Ceased WO1995002584A2 (en)

Priority Applications (15)

Application Number Priority Date Filing Date Title
NZ269904A NZ269904A (en) 1993-07-16 1994-07-11 1,3-oxazole derivatives; preparative process; intermediate compounds
EP94922511A EP0708762B1 (en) 1993-07-16 1994-07-11 Process for making hiv protease inhibitors
DE69426979T DE69426979T2 (en) 1993-07-16 1994-07-11 METHOD FOR PRODUCING HIV PROTEASE INHIBITORS
JP50463295A JP3547136B2 (en) 1993-07-16 1994-07-11 Method for producing HIV protease inhibitor
AU73588/94A AU676079B2 (en) 1993-07-16 1994-07-11 Process for making HIV protease inhibitors
AT94922511T ATE200079T1 (en) 1993-07-16 1994-07-11 METHOD FOR PRODUCING HIV PROTEASE INHIBITORS
DK94922511T DK0708762T3 (en) 1993-07-16 1994-07-11 Method of Preparation of HIV Protease Inhibitors
CA002167183A CA2167183C (en) 1993-07-16 1994-07-11 Process for making hiv protease inhibitors
RU96103642A RU2125561C1 (en) 1993-07-16 1994-07-11 Intermediate compounds for synthesis of hiv-protease inhibitors and a method of their synthesis
SK55-96A SK282616B6 (en) 1993-07-16 1994-07-11 Production method for intermediates for production of hiv-proteas e inhibitors and relevant intermediates
KR1019960700208A KR100329694B1 (en) 1993-07-16 1994-07-11 Method for preparing human immunodeficiency virus (HIV) protease inhibitor
PL94312613A PL179039B1 (en) 1993-07-16 1994-07-11 Methods of producing intermediate compounds for HIV protease inhibitors and a new PL PL PL indirect compound
NO960168A NO306297B1 (en) 1993-07-16 1996-01-15 Method of Preparation of HIV Protease Inhibitors
FI960184A FI119473B (en) 1993-07-16 1996-01-15 Process for the manufacture of HIV protease inhibitors
GR20010400119T GR3035645T3 (en) 1993-07-16 2001-03-29 Process for making hiv protease inhibitors

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US9322593A 1993-07-16 1993-07-16
US093,225 1993-07-16
US08/187,664 US5463067A (en) 1993-07-16 1994-01-26 Process for making HIV protease inhibitors
US187,664 1994-01-26

Publications (2)

Publication Number Publication Date
WO1995002584A2 WO1995002584A2 (en) 1995-01-26
WO1995002584A3 true WO1995002584A3 (en) 1995-03-09

Family

ID=26787287

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US1994/007706 Ceased WO1995002584A2 (en) 1993-07-16 1994-07-11 Process for making hiv protease inhibitors

Country Status (22)

Country Link
US (2) US5491238A (en)
EP (1) EP0708762B1 (en)
JP (1) JP3547136B2 (en)
CN (2) CN1066723C (en)
AT (1) ATE200079T1 (en)
AU (1) AU676079B2 (en)
CZ (1) CZ293953B6 (en)
DE (1) DE69426979T2 (en)
DK (1) DK0708762T3 (en)
ES (1) ES2155091T3 (en)
FI (1) FI119473B (en)
GR (1) GR3035645T3 (en)
HU (1) HUT74583A (en)
IL (1) IL110342A (en)
LV (1) LV12825B (en)
NO (1) NO306297B1 (en)
NZ (1) NZ269904A (en)
PL (1) PL179039B1 (en)
PT (1) PT708762E (en)
RU (1) RU2125561C1 (en)
SK (1) SK282616B6 (en)
WO (1) WO1995002584A2 (en)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL110255A (en) * 1993-07-16 1998-12-06 Merck & Co Inc Formation and resolution of 2-tert-butylcarboxamido-piperazine
IL111584A0 (en) * 1993-11-18 1995-01-24 Merck & Co Inc Prodrugs of an inhibitor of hiv protease and pharmaceutical compositions containing them
EP0710652B1 (en) * 1994-11-04 1998-03-04 Yamakawa Chemical Industry Co., Ltd. Process for preparing optically active piperazine derivatives and intermediates for preparation
DE4446025A1 (en) * 1994-12-22 1996-06-27 Basf Ag 2-caroxamido-1,4,5,6-tetrahydropyrazine
EP1125930A1 (en) * 1995-05-23 2001-08-22 Lonza Ag Optically active piperazine-2-carboxylic acid derivatives and process for their preparation
EP0744401B1 (en) * 1995-05-23 2001-11-21 Lonza Ag Process for the preparation of optically active 2-piperazine carboxylic acid derivatives
CA2201218C (en) * 1996-04-23 2004-09-28 Rudolf Fuchs Process for the preparation of optically active piperazine-2-carboxylic acid derivatives
US6645961B1 (en) 1997-03-07 2003-11-11 Merck & Co., Inc. Dry granulation formulation for an HIV protease inhibitor
US6482952B2 (en) 2000-06-20 2002-11-19 Merck & Co., Inc. Process for preparing acetonides
US7218837B2 (en) 2000-09-25 2007-05-15 Victor Company Of Japan, Ltd. Program-signal recording and reproducing apparatus

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0480714A2 (en) * 1990-10-11 1992-04-15 Merck & Co. Inc. HIV protease inhibitors having symmetrical structure
US5169952A (en) * 1991-07-02 1992-12-08 Merck & Co., Inc. Stereoselective production of hydroxyamide compounds from chiral α-amino epoxides
EP0521686A1 (en) * 1991-07-02 1993-01-07 Merck & Co. Inc. Stereoselective production of hydroxyamide compounds from chiral a-amino epoxides

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0480714A2 (en) * 1990-10-11 1992-04-15 Merck & Co. Inc. HIV protease inhibitors having symmetrical structure
US5169952A (en) * 1991-07-02 1992-12-08 Merck & Co., Inc. Stereoselective production of hydroxyamide compounds from chiral α-amino epoxides
EP0521686A1 (en) * 1991-07-02 1993-01-07 Merck & Co. Inc. Stereoselective production of hydroxyamide compounds from chiral a-amino epoxides

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
B.D. DORSEY ET AL.: "A Concise and Enantioselective Synthesis of Novel HIV-1 Protease Transition state Mimics", TETRAHEDRON LETTERS, vol. 34, no. 12, 1993, pages 1851 - 1854 *
D. ASKIN ET AL.: "Highly Diastereoselective Alkylations of Chiral Amide Enolates: New Routes to Hydroxyethylene Dipeptide Isostere Inhibitors of HIV-1 Protease", J. ORG. CHEM., vol. 57, no. 10, 1992, pages 2771 - 2773 *

Also Published As

Publication number Publication date
JPH08509985A (en) 1996-10-22
NO960168L (en) 1996-03-15
EP0708762B1 (en) 2001-03-28
US5496948A (en) 1996-03-05
FI119473B (en) 2008-11-28
NZ269904A (en) 1997-11-24
HUT74583A (en) 1997-01-28
PL312613A1 (en) 1996-04-29
ATE200079T1 (en) 2001-04-15
GR3035645T3 (en) 2001-06-29
LV12825A (en) 2002-05-20
WO1995002584A2 (en) 1995-01-26
CN1066723C (en) 2001-06-06
DE69426979T2 (en) 2001-09-20
CN1192014C (en) 2005-03-09
PL179039B1 (en) 2000-07-31
SK282616B6 (en) 2002-10-08
HU9600077D0 (en) 1996-03-28
CN1130380A (en) 1996-09-04
DK0708762T3 (en) 2001-04-30
IL110342A0 (en) 1994-10-21
IL110342A (en) 1998-12-27
CZ13196A3 (en) 1996-04-17
CZ293953B6 (en) 2004-08-18
FI960184A0 (en) 1996-01-15
RU2125561C1 (en) 1999-01-27
JP3547136B2 (en) 2004-07-28
NO960168D0 (en) 1996-01-15
AU676079B2 (en) 1997-02-27
SK5596A3 (en) 1997-01-08
CN1252402A (en) 2000-05-10
EP0708762A1 (en) 1996-05-01
PT708762E (en) 2001-07-31
LV12825B (en) 2002-09-20
FI960184L (en) 1996-03-14
AU7358894A (en) 1995-02-13
NO306297B1 (en) 1999-10-18
DE69426979D1 (en) 2001-05-03
ES2155091T3 (en) 2001-05-01
US5491238A (en) 1996-02-13

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