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
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.)
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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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic 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
    • C07D295/04—Heterocyclic 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
    • C07D295/08—Heterocyclic 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
    • C07D295/096—Heterocyclic 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
    • 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
    • A61P31/04—Antibacterial agents
    • 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
    • A61P31/10—Antimycotics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic 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
    • C07D207/04—Heterocyclic 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
    • C07D207/08—Heterocyclic 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
    • C07D207/09—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic 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
    • C07D231/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic 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
    • C07D233/56—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/10—1,2,4-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
    • C07D249/12—Oxygen 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)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Communicable Diseases (AREA)
  • Animal Behavior & Ethology (AREA)
  • Oncology (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

ID=27120397

Family Applications (1)

Application Number Title Priority Date Filing Date
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

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

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
ZA9410142B (en) * 1993-12-21 1996-05-02 Schering Corp Tetrahydrofuran antifungals
US5693626A (en) * 1993-12-21 1997-12-02 Schering Corporation Tetrahydrofuran antifungals
US5661151A (en) * 1993-12-21 1997-08-26 Schering Corporation Tetrahydrofuran antifungals
US5710154A (en) * 1993-12-21 1998-01-20 Schering Corporation Tetrahydrofuran antifungals
US5703236A (en) * 1993-12-21 1997-12-30 Schering Corporation Tetrahydrofuran antifungals
US5714490A (en) * 1993-12-21 1998-02-03 Schering Corporation Tetrahydrofuran antifungals
US5703079A (en) * 1993-12-21 1997-12-30 Schering Corporation Tetrahydrofuran antifungals
WO1995019983A1 (en) * 1994-01-24 1995-07-27 Janssen Pharmaceutica N.V. Watersoluble azole antifungals
KR960703103A (ko) * 1994-04-19 1996-06-19 후루따 다께시 트리아졸 유도체의 제조방법(process for producing triazole derivative)
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
WO1996002664A1 (en) * 1994-07-18 1996-02-01 Daicel Chemical Industries, Ltd. Process for producing optically active triazole compound and method of racemizing optically active triazole compound
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
MX9701229A (es) * 1995-06-02 1997-05-31 Schering Corp Antifungicos de tetrahidrofurano.
US5698557A (en) * 1995-06-19 1997-12-16 Schering Corporation Hydroxy-substituted antifungals
WO1997000255A1 (en) * 1995-06-19 1997-01-03 Schering Corporation 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
JP2001519346A (ja) * 1997-10-07 2001-10-23 シェーリング コーポレイション 抗真菌性結晶性多形物
BR0215702A (pt) * 2002-04-12 2005-10-18 Ranbaxy Lab Ltd Derivados de tetraidrofurano 2,2,4-trisubstituìdo como agentes antifúngicos
US9073904B2 (en) 2010-05-19 2015-07-07 Sandoz Ag Preparation of posaconazole intermediates
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
BR112012029225B1 (pt) 2010-05-19 2020-10-27 Sandoz Ag processo para a preparação de um composto quiral, composto quiral e uso de um composto quiral
US9206146B2 (en) 2010-05-19 2015-12-08 Sandoz Ag Purification of posaconazole and of posaconazole intermediates
WO2012172015A1 (en) 2011-06-16 2012-12-20 Sandoz Ag Process for the preparation of a chiral compound
KR102240329B1 (ko) * 2013-06-07 2021-04-14 더 스크립스 리서치 인스티튜트 섬유증의 소분자 억제제
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
US5006513A (en) 1987-11-09 1991-04-09 Miles Inc. Antimycotic compositions of nikkomycin compounds and azole antimycotica
ATE115577T1 (de) 1987-11-20 1994-12-15 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
US5039676A (en) 1990-05-11 1991-08-13 Schering Corporation Tri- and tetra-substituted-oxetanes and tetrahydrofurans and intermediates thereof
US20040220100A1 (en) 2000-07-21 2004-11-04 Essentia Biosystems, Inc. Multi-component biological transport systems

Patent 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

Also Published As

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

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