AU2007245194B2 - Process for preparation of HIV protease inhibitors - Google Patents

Process for preparation of HIV protease inhibitors Download PDF

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Publication number
AU2007245194B2
AU2007245194B2 AU2007245194A AU2007245194A AU2007245194B2 AU 2007245194 B2 AU2007245194 B2 AU 2007245194B2 AU 2007245194 A AU2007245194 A AU 2007245194A AU 2007245194 A AU2007245194 A AU 2007245194A AU 2007245194 B2 AU2007245194 B2 AU 2007245194B2
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AU
Australia
Prior art keywords
formula
compound
combining
ome
tbuo
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AU2007245194A
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English (en)
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AU2007245194A1 (en
Inventor
Kenneth R. Crawford
Eric D. Dowdy
Arnold Gutierrez
Richard P. Polniaszek
Richard Hung Chiu Yu
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Gilead Sciences Inc
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Gilead Sciences Inc
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Publication of AU2007245194A1 publication Critical patent/AU2007245194A1/en
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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C327/00—Thiocarboxylic acids
    • C07C327/38—Amides of thiocarboxylic acids
    • C07C327/40—Amides of thiocarboxylic acids having carbon atoms of thiocarboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C327/42—Amides of thiocarboxylic acids having carbon atoms of thiocarboxamide groups bound to hydrogen atoms or to acyclic carbon atoms to hydrogen atoms or to carbon atoms of a saturated carbon skeleton
    • 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
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
    • A61K31/665—Phosphorus compounds having oxygen as a ring hetero atom, e.g. fosfomycin
    • 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
    • A61P31/12—Antivirals
    • 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
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C253/00—Preparation of carboxylic acid nitriles
    • C07C253/30—Preparation of carboxylic acid nitriles by reactions not involving the formation of cyano groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C303/00—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
    • C07C303/36—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of amides of sulfonic acids
    • C07C303/38—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of amides of sulfonic acids by reaction of ammonia or amines with sulfonic acids, or with esters, anhydrides, or halides thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C303/00—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
    • C07C303/36—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of amides of sulfonic acids
    • C07C303/40—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of amides of sulfonic acids by reactions not involving the formation of sulfonamide groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/22—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms
    • C07C311/29—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/41—Preparation of salts of carboxylic acids
    • C07C51/412—Preparation of salts of carboxylic acids by conversion of the acids, their salts, esters or anhydrides with the same carboxylic acid part
    • 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
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • 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
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/40—Esters thereof
    • C07F9/4003—Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4006—Esters of acyclic acids which can have further substituents on alkyl
    • 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
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/40—Esters thereof
    • C07F9/4071—Esters thereof the ester moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4075—Esters with hydroxyalkyl compounds
    • 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
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/40—Esters thereof
    • C07F9/4071—Esters thereof the ester moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4084—Esters with hydroxyaryl compounds

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Virology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Medicinal Preparation (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2007245194A 2006-03-29 2007-03-29 Process for preparation of HIV protease inhibitors Active AU2007245194B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US78712606P 2006-03-29 2006-03-29
US60/787,126 2006-03-29
PCT/US2007/007564 WO2007126812A2 (en) 2006-03-29 2007-03-29 Process for preparation of hiv protease inhibitors

Publications (2)

Publication Number Publication Date
AU2007245194A1 AU2007245194A1 (en) 2007-11-08
AU2007245194B2 true AU2007245194B2 (en) 2013-03-14

Family

ID=38323963

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2007245194A Active AU2007245194B2 (en) 2006-03-29 2007-03-29 Process for preparation of HIV protease inhibitors

Country Status (24)

Country Link
US (4) US20110065631A1 (enExample)
EP (2) EP2570416B1 (enExample)
JP (2) JP5430395B2 (enExample)
KR (2) KR101429300B1 (enExample)
CN (2) CN102516259B (enExample)
AP (2) AP2013006690A0 (enExample)
AU (1) AU2007245194B2 (enExample)
BR (1) BRPI0710199A2 (enExample)
CA (1) CA2647316C (enExample)
DK (1) DK1999133T3 (enExample)
EA (2) EA020088B1 (enExample)
ES (2) ES2430557T3 (enExample)
HR (2) HRP20080554B1 (enExample)
IL (2) IL194122A (enExample)
MX (1) MX2008012398A (enExample)
NO (2) NO342102B1 (enExample)
NZ (2) NZ596074A (enExample)
PL (1) PL1999133T3 (enExample)
PT (1) PT1999133E (enExample)
SG (1) SG170794A1 (enExample)
SI (1) SI1999133T1 (enExample)
UA (1) UA97241C2 (enExample)
WO (1) WO2007126812A2 (enExample)
ZA (1) ZA200808046B (enExample)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8921415B2 (en) 2009-01-29 2014-12-30 Mapi Pharma Ltd. Polymorphs of darunavir
AU2011210349A1 (en) 2010-01-28 2012-07-05 Mapi Pharma Limited Process for the preparation of darunavir and darunavir intermediates
CN102190638A (zh) * 2010-03-16 2011-09-21 中国科学院上海药物研究所 联芳基醇二胺类化合物、其药物组合物、制备方法及应用
CN102584748B (zh) * 2011-01-13 2015-02-11 浙江九洲药业股份有限公司 夫沙那韦中间体的制备方法
ES2655525T3 (es) * 2011-04-26 2018-02-20 Mylan Laboratories Ltd. Proceso novedoso para la preparación de Etravirina
EP2634180A1 (en) 2012-03-01 2013-09-04 Lonza Ltd. Enzymatic process for the preparation of butyrolactones
PT2764002T (pt) * 2014-04-11 2018-05-16 Gilead Sciences Inc Métodos para a preparação de análogos de nucleótidos anti-virais
CN103664976B (zh) * 2013-12-12 2015-11-04 惠州市莱佛士制药技术有限公司 一种顺式六氢呋喃并[2,3-b]呋喃-3-醇的制备方法
ES2802376T3 (es) * 2014-02-12 2021-01-19 Firmenich Incorporated Procedimiento mejorado para la síntesis de 1-bencil-3-(1-(isoxazol-4-ilmetil)-1h-pirazol-4-il)imidazolidin-2,4-dionas sustituidas
SG11201705069YA (en) 2014-12-26 2017-07-28 Univ Emory N4-hydroxycytidine and derivatives and anti-viral uses related thereto
JP6435907B2 (ja) * 2015-02-16 2018-12-12 住友化学株式会社 ヘキサヒドロフロフラノール誘導体の製造方法
CN108610227B (zh) * 2016-12-10 2021-02-09 中国科学院大连化学物理研究所 一种制备双环芳香化合物的方法
PL3706762T3 (pl) 2017-12-07 2025-02-10 Emory University N4-hydroksycytydyna i pochodne oraz związane z nimi zastosowania przeciwwirusowe
SG11202107145SA (en) 2019-01-25 2021-08-30 Univ Brown Compositions and methods for treating, preventing or reversing age-associated inflammation and disorders

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002067239A2 (en) * 2000-10-24 2002-08-29 Glaxo Group Limited Process for preparing intermediates of hiv protease inhibitors

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1994026749A1 (en) * 1993-05-14 1994-11-24 Merck & Co., Inc. Hiv protease inhibitors
AU1369001A (en) * 1995-12-13 2001-03-22 Abbott Laboratories Retroviral protease inhibiting compounds
EP2314564A3 (en) 1999-12-23 2012-04-04 Ampac Fine Chemicals LLC Improved preparation of 2S,3S-N-isobutyl-N-(2-hydroxy-3-amino-4-phenylbutyl)-p-nitrobenzenesulfonylamide hydrochloride and other derivatives of 2-hydroxy-1,3-diamines
EP1436884A2 (en) 2001-07-20 2004-07-14 Koninklijke Philips Electronics N.V. Oscillating circuit, converter with such oscillating circuit, and preconditioner with such converter
TWI332956B (en) * 2002-04-26 2010-11-11 Gilead Sciences Inc Cellular accumulation of phosphonate analogs of hiv protease inhibitor compounds
US20050239054A1 (en) * 2002-04-26 2005-10-27 Arimilli Murty N Method and compositions for identifying anti-HIV therapeutic compounds
AU2004286239A1 (en) * 2003-10-24 2005-05-12 Gilead Sciences, Inc. Methods and compositions for identifying therapeutic compounds

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002067239A2 (en) * 2000-10-24 2002-08-29 Glaxo Group Limited Process for preparing intermediates of hiv protease inhibitors

Also Published As

Publication number Publication date
AP2013006690A0 (en) 2013-01-31
CA2647316A1 (en) 2007-11-08
DK1999133T3 (da) 2013-11-25
EA016140B1 (ru) 2012-02-28
US8173623B2 (en) 2012-05-08
US20110065631A1 (en) 2011-03-17
CN102516259A (zh) 2012-06-27
AP2008004641A0 (en) 2008-10-31
KR101429300B1 (ko) 2014-08-11
NO342102B1 (no) 2018-03-26
HRP20140626A2 (hr) 2014-11-07
EP1999133B1 (en) 2013-08-21
KR20080108322A (ko) 2008-12-12
US20120258935A1 (en) 2012-10-11
HRP20080554A2 (hr) 2009-02-28
IL194122A (en) 2016-08-31
CN101448838A (zh) 2009-06-03
CN102516259B (zh) 2014-12-10
JP5430395B2 (ja) 2014-02-26
JP2009531441A (ja) 2009-09-03
PT1999133E (pt) 2013-10-16
US20130172295A1 (en) 2013-07-04
UA97241C2 (uk) 2012-01-25
KR20140021047A (ko) 2014-02-19
KR101395377B1 (ko) 2014-05-14
AP2757A (en) 2013-09-30
HRP20080554B1 (hr) 2014-11-21
US20080004242A1 (en) 2008-01-03
BRPI0710199A2 (pt) 2012-03-06
HK1126756A1 (en) 2009-09-11
SI1999133T1 (sl) 2013-10-30
WO2007126812A3 (en) 2007-12-21
NZ571302A (en) 2011-11-25
PL1999133T3 (pl) 2014-01-31
EA201100994A1 (ru) 2012-03-30
EP2570416B1 (en) 2016-03-16
NO20084547L (no) 2008-12-22
NO342965B1 (no) 2018-09-10
HK1180311A1 (en) 2013-10-18
ZA200808046B (en) 2009-06-24
MX2008012398A (es) 2008-12-17
ES2430557T3 (es) 2013-11-21
JP2013082717A (ja) 2013-05-09
CN101448838B (zh) 2012-07-04
US8431745B2 (en) 2013-04-30
EA020088B1 (ru) 2014-08-29
EP1999133A2 (en) 2008-12-10
EA200802074A1 (ru) 2009-02-27
ES2572001T3 (es) 2016-05-27
NZ596074A (en) 2013-03-28
EP2570416A1 (en) 2013-03-20
WO2007126812A2 (en) 2007-11-08
SG170794A1 (en) 2011-05-30
NO20180086A1 (no) 2008-12-22
IL225167A (en) 2016-03-31
CA2647316C (en) 2013-05-28
AU2007245194A1 (en) 2007-11-08

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