CN1037267C - 制备三取代四氢呋喃衍生物的方法 - Google Patents

制备三取代四氢呋喃衍生物的方法 Download PDF

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Publication number
CN1037267C
CN1037267C CN92113399A CN92113399A CN1037267C CN 1037267 C CN1037267 C CN 1037267C CN 92113399 A CN92113399 A CN 92113399A CN 92113399 A CN92113399 A CN 92113399A CN 1037267 C CN1037267 C CN 1037267C
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CN
China
Prior art keywords
compound
triazol
formula
phenyl
difluorophenyl
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Expired - Fee Related
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CN92113399A
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English (en)
Chinese (zh)
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CN1073944A (zh
Inventor
A·K·沙森纳
V·M·吉里扎瓦拉汉
A·K·冈古利
R·G·洛维
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Merck Sharp and Dohme LLC
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Schering Corp
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/08Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
    • C07D295/096Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10Antimycotics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • C07D207/09Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/101,2,4-Triazoles; Hydrogenated 1,2,4-triazoles 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
    • C07D249/12Oxygen or sulfur atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Communicable Diseases (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Saccharide Compounds (AREA)
CN92113399A 1991-10-30 1992-10-29 制备三取代四氢呋喃衍生物的方法 Expired - Fee Related CN1037267C (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US78535791A 1991-10-30 1991-10-30
US785,357 1991-10-30
US90726292A 1992-07-01 1992-07-01
US907,262 1992-07-01

Publications (2)

Publication Number Publication Date
CN1073944A CN1073944A (zh) 1993-07-07
CN1037267C true CN1037267C (zh) 1998-02-04

Family

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Family Applications (1)

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CN92113399A Expired - Fee Related CN1037267C (zh) 1991-10-30 1992-10-29 制备三取代四氢呋喃衍生物的方法

Country Status (22)

Country Link
EP (2) EP0610377B1 (https=)
JP (1) JP3210017B2 (https=)
CN (1) CN1037267C (https=)
AT (1) ATE198888T1 (https=)
AU (1) AU665218B2 (https=)
CA (1) CA2122270C (https=)
CZ (1) CZ102794A3 (https=)
DE (1) DE69231661T2 (https=)
ES (1) ES2153364T3 (https=)
FI (1) FI941986A7 (https=)
HR (1) HRP921145A2 (https=)
HU (1) HUT70742A (https=)
IL (1) IL103558A0 (https=)
MX (1) MX9206222A (https=)
MY (1) MY109529A (https=)
NO (1) NO941589L (https=)
NZ (1) NZ244910A (https=)
SG (1) SG42920A1 (https=)
SI (1) SI9200285A (https=)
SK (1) SK48894A3 (https=)
WO (1) WO1993009114A1 (https=)
YU (1) YU94792A (https=)

Families Citing this family (31)

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US5403937A (en) * 1993-04-30 1995-04-04 Schering Corporation Process for preparing intermediates for the synthesis of antifungal agents
US5349099A (en) * 1993-12-13 1994-09-20 Schering Corporation Process for preparing intermediates for the synthesis of antifungal agents
US5693626A (en) * 1993-12-21 1997-12-02 Schering Corporation Tetrahydrofuran antifungals
US5661151A (en) * 1993-12-21 1997-08-26 Schering Corporation Tetrahydrofuran antifungals
PL181193B1 (pl) * 1993-12-21 2001-06-29 Schering Corp Nowe pochodne tetrahydrofuranowe o działaniu przeciwgrzybicznym, kompozycja farmaceutyczna do leczenia infekcji grzybiczych oraz sposób wytwarzania tych związków
US5703236A (en) * 1993-12-21 1997-12-30 Schering Corporation Tetrahydrofuran antifungals
US5710154A (en) * 1993-12-21 1998-01-20 Schering Corporation Tetrahydrofuran antifungals
US5703079A (en) * 1993-12-21 1997-12-30 Schering Corporation Tetrahydrofuran antifungals
US5714490A (en) * 1993-12-21 1998-02-03 Schering Corporation Tetrahydrofuran antifungals
SG48386A1 (en) * 1994-01-24 1998-04-17 Janssen Pharmaceutica Nv Watersoluble azole antifungals
JP3828147B2 (ja) * 1994-04-19 2006-10-04 株式会社カネカ トリアゾール誘導体の製造法
US5442093A (en) * 1994-05-09 1995-08-15 Schering Corporation Process for preparing intermediates for the synthesis of antifungal agents
US5486625A (en) * 1994-07-08 1996-01-23 Schering Corporation Process for the preparation of chiral intermediates useful for the synthesis of antifungal agents
US5702928A (en) * 1994-07-18 1997-12-30 Daicel Chemical Industries, Ltd. Process for producing optically active triazole compounds and method of racemizing optically active triazole compounds
US5616777A (en) * 1995-04-19 1997-04-01 Schering Corporation Chiral hydrazine derivatives
US5625064A (en) * 1995-04-19 1997-04-29 Schering Corporation Process for the preparation of triazolones
HUP9701690A3 (en) * 1995-06-02 1998-04-28 Schering Corp Kenilwort Tetrahydrofuran derivatives as antifungals and pharmaceutical compositions containing the same
US5698557A (en) * 1995-06-19 1997-12-16 Schering Corporation Hydroxy-substituted antifungals
IL118668A0 (en) * 1995-06-19 1996-10-16 Schering Corp Tetrahydrofuran antifungals
US5834472A (en) * 1996-05-24 1998-11-10 Schering Corporation Antifungal composition with enhanced bioavailability
US5846971A (en) * 1996-06-28 1998-12-08 Schering Corporation Oral antifungal composition
TW593312B (en) 1997-07-11 2004-06-21 Janssen Pharmaceutica Nv 2,4,4-trisubstituted-1,3-dioxolane antifungals
KR100626109B1 (ko) * 1997-10-07 2006-09-20 쉐링 코포레이션 항진균성 결정성 다형체 및 이를 포함하는 약제학적 조성물
BR0215702A (pt) * 2002-04-12 2005-10-18 Ranbaxy Lab Ltd Derivados de tetraidrofurano 2,2,4-trisubstituìdo como agentes antifúngicos
JP5955837B2 (ja) 2010-05-19 2016-07-20 サンド・アクチエンゲゼルシヤフト ポサコナゾール及びポサコナゾール中間体の精製
EP2571847B1 (en) 2010-05-19 2016-09-21 Sandoz AG Process for the preparation of chiral hydrazides
CN102906087B (zh) 2010-05-19 2016-03-23 桑多斯股份公司 制备手性三唑酮的方法
AU2011254657B2 (en) 2010-05-19 2016-02-04 Sandoz Ag Preparation of posaconazole intermediates
CA2838051C (en) 2011-06-16 2019-09-24 Sandoz Ag Process for the preparation of a chiral compound
EP3626242B1 (en) * 2013-06-07 2024-08-07 The Scripps Research Institute Itraconazole analogs as inhibitors of fibrosis
CN106397417A (zh) * 2016-08-30 2017-02-15 甘肃皓天化学科技有限公司 用于制备泊沙康唑的中间体的制备方法

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0173258A2 (de) * 1984-08-31 1986-03-05 F. HOFFMANN-LA ROCHE & CO. Aktiengesellschaft Substituierte 2-Phenyl-1,3-dioxolane
EP0283992A2 (en) * 1987-03-25 1988-09-28 Janssen Pharmaceutica N.V. 4-[4-[4-[4-[[2-(2,4-Difluorophenyl)-2-(1H-azolylmethyl)-1,3-dioxolan-4-yl]-methoxy]phenyl]-1-piperazinyl]phenyl]triazolones
EP0402989A2 (en) * 1989-06-09 1990-12-19 Janssen Pharmaceutica N.V. Antifungal 4-[4-[4-[4-[[2-(2,4-difluorophenyl)-2-(1H-azolylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-1-piperazinyl]phenyl]triazolones and imidazolones

Family Cites Families (10)

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US4267179A (en) * 1978-06-23 1981-05-12 Janssen Pharmaceutica, N.V. Heterocyclic derivatives of (4-phenylpiperazin-1-yl-aryloxymethyl-1,3-dioxolan-2-yl)methyl-1H-imidazoles and 1H-1,2,4-triazoles
US4619931A (en) * 1983-02-28 1986-10-28 Janssen Pharmaceutica, N.V. [[4-[4-(4-phenyl-1-piperazinyl)phenoxymethyl]-1,3-dioxolan-2-yl]methyl]-1H-imidazoles and 1H-1,2,4-triazoles
DE3346123A1 (de) 1983-12-21 1985-06-27 Janssen Pharmaceutica, N.V., Beerse Pharmazeutische praeparate von in wasser schwerloeslichen oder instabilen arzneistoffen und verfahren zu ihrer herstellung
US4727064A (en) 1984-04-25 1988-02-23 The United States Of America As Represented By The Department Of Health And Human Services Pharmaceutical preparations containing cyclodextrin derivatives
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DE3852477T2 (de) * 1987-11-20 1995-05-04 Schering Corp Tri- und tetrasubstituierte Oxetane und Tetrahydrofurane und deren Zwischenprodukte.
US5002935A (en) 1987-12-30 1991-03-26 University Of Florida Improvements in redox systems for brain-targeted drug delivery
CA1331757C (en) * 1988-02-29 1994-08-30 Janssen Pharmaceutica Naamloze Vennootschap 5-lipoxygenase inhibiting 4-(4-phenyl-1-piperazinyl)phenols
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Patent Citations (3)

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Publication number Priority date Publication date Assignee Title
EP0173258A2 (de) * 1984-08-31 1986-03-05 F. HOFFMANN-LA ROCHE & CO. Aktiengesellschaft Substituierte 2-Phenyl-1,3-dioxolane
EP0283992A2 (en) * 1987-03-25 1988-09-28 Janssen Pharmaceutica N.V. 4-[4-[4-[4-[[2-(2,4-Difluorophenyl)-2-(1H-azolylmethyl)-1,3-dioxolan-4-yl]-methoxy]phenyl]-1-piperazinyl]phenyl]triazolones
EP0402989A2 (en) * 1989-06-09 1990-12-19 Janssen Pharmaceutica N.V. Antifungal 4-[4-[4-[4-[[2-(2,4-difluorophenyl)-2-(1H-azolylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-1-piperazinyl]phenyl]triazolones and imidazolones

Also Published As

Publication number Publication date
EP0610377A1 (en) 1994-08-17
SG42920A1 (en) 1997-10-17
CZ102794A3 (en) 1995-03-15
WO1993009114A1 (en) 1993-05-13
NO941589D0 (https=) 1994-04-29
SK48894A3 (en) 1995-02-08
AU2916992A (en) 1993-06-07
CA2122270C (en) 2006-05-23
MX9206222A (es) 1993-04-01
EP0539938A1 (en) 1993-05-05
AU665218B2 (en) 1995-12-21
IL103558A0 (en) 1993-03-15
HU9401256D0 (en) 1994-08-29
FI941986A0 (fi) 1994-04-29
DE69231661D1 (de) 2001-03-01
CN1073944A (zh) 1993-07-07
EP0610377B1 (en) 2001-01-24
CA2122270A1 (en) 1993-05-13
SI9200285A (en) 1993-06-30
NO941589L (https=) 1994-06-23
ATE198888T1 (de) 2001-02-15
FI941986A7 (fi) 1994-04-29
ES2153364T3 (es) 2001-03-01
NZ244910A (en) 1996-01-26
YU94792A (sh) 1995-12-04
JP3210017B2 (ja) 2001-09-17
JPH07500605A (ja) 1995-01-19
HUT70742A (en) 1995-10-30
MY109529A (en) 1997-02-28
DE69231661T2 (de) 2001-08-02
HRP921145A2 (en) 1994-08-31

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