MX9801025A - Preparacion de triazoles mediante adicion organometalica a cetonas e intermediarios de los mismos. - Google Patents

Preparacion de triazoles mediante adicion organometalica a cetonas e intermediarios de los mismos.

Info

Publication number
MX9801025A
MX9801025A MX9801025A MX9801025A MX9801025A MX 9801025 A MX9801025 A MX 9801025A MX 9801025 A MX9801025 A MX 9801025A MX 9801025 A MX9801025 A MX 9801025A MX 9801025 A MX9801025 A MX 9801025A
Authority
MX
Mexico
Prior art keywords
compound
formula
preparation
triazoles
ketones
Prior art date
Application number
MX9801025A
Other languages
English (en)
Inventor
Michael Butters
Julien Ann Harrison
Alan John Pettman
Original Assignee
Pfizer Res & Dev
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=10778850&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=MX9801025(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Pfizer Res & Dev filed Critical Pfizer Res & Dev
Publication of MX9801025A publication Critical patent/MX9801025A/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/30—Halogen atoms or nitro radicals
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • 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
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/34—One oxygen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/34—One oxygen atom
    • C07D239/36—One oxygen atom as doubly bound oxygen atom or as unsubstituted hydroxy radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Epidemiology (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)

Abstract

La invencion proporciona un procedimiento para preparar un compuesto de formula (Ver Formula) o una de sus sales de adicion de ácidos o de base, en la que R es fenilo opcionalmente sustituido por 1 a 3 sustituyentes, seleccionados cada uno independientemente entre halo y trifluorometilo; R1 es alquilo de C1-C6; y "Het" es pirimidinilo opcionalmente sustituido por 1 a 3 sustituyentes, seleccionados cada uno independientemente entre alquilo de C1-C4, alcoxi de C1-C4, halo, oxo, bencilo y benciloxi, que comprende la reaccion de un compuesto de formula (Ver Formula).
MX9801025A 1995-08-05 1996-07-26 Preparacion de triazoles mediante adicion organometalica a cetonas e intermediarios de los mismos. MX9801025A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB9516121.2A GB9516121D0 (en) 1995-08-05 1995-08-05 Organometallic addition to ketones
PCT/EP1996/003376 WO1997006160A1 (en) 1995-08-05 1996-07-26 Preparation of triazoles by organometallic addition to ketones and intermediates therefor

Publications (1)

Publication Number Publication Date
MX9801025A true MX9801025A (es) 1998-04-30

Family

ID=10778850

Family Applications (1)

Application Number Title Priority Date Filing Date
MX9801025A MX9801025A (es) 1995-08-05 1996-07-26 Preparacion de triazoles mediante adicion organometalica a cetonas e intermediarios de los mismos.

Country Status (32)

Country Link
US (2) US6586594B1 (es)
EP (1) EP0871625B1 (es)
JP (3) JP3211965B2 (es)
KR (1) KR100269048B1 (es)
CN (1) CN1076019C (es)
AR (1) AR003472A1 (es)
AT (1) ATE256679T1 (es)
AU (1) AU703337B2 (es)
BR (1) BR9609960A (es)
CA (1) CA2228655C (es)
CZ (1) CZ296975B6 (es)
DE (1) DE69631160T2 (es)
DK (1) DK0871625T3 (es)
EG (1) EG21200A (es)
ES (1) ES2210382T3 (es)
GB (1) GB9516121D0 (es)
HK (1) HK1014944A1 (es)
HU (1) HU224339B1 (es)
IL (2) IL131521A (es)
IN (1) IN190817B (es)
MX (1) MX9801025A (es)
MY (1) MY123062A (es)
NO (1) NO314938B1 (es)
NZ (1) NZ315651A (es)
PE (1) PE16897A1 (es)
PL (1) PL187227B1 (es)
PT (1) PT871625E (es)
RU (1) RU2156760C2 (es)
TR (1) TR199800170T1 (es)
TW (1) TW442480B (es)
WO (1) WO1997006160A1 (es)
ZA (1) ZA966587B (es)

Families Citing this family (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7193083B2 (en) * 1996-07-26 2007-03-20 Pfizer, Inc. Preparation of triazoles by organometallic addition to ketones and intermediates therefor
TWI329105B (en) * 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
DE60330466D1 (de) 2002-07-29 2010-01-21 Rigel Pharmaceuticals Inc VERFAHREN ZUR BEHANDLUNG ODER PRuVENTION VON AUTOIMMUNKRANKHEITEN MIT 2,4-PYRIMIDINDIAMIN-VERBINDUNGEN
NZ545270A (en) 2003-07-30 2010-04-30 Rigel Pharmaceuticals Inc 2,4-Pyrimidinediamine compounds for use in the treatment or prevention of autoimmune diseases
US20060058525A1 (en) * 2004-09-01 2006-03-16 Rajinder Singh Synthesis of 2,4-pyrimidinediamine compounds
ES2380550T3 (es) * 2004-11-24 2012-05-16 Rigel Pharmaceuticals, Inc. Compuestos de espiro-2,4-pirimidindiamina y sus usos
EP1828170A4 (en) * 2004-12-14 2009-11-11 Reddys Lab Ltd Dr PROCESS FOR PREPARING VORICONAZOLE
US20060270694A1 (en) * 2005-05-03 2006-11-30 Rigel Pharmaceuticals, Inc. JAK kinase inhibitors and their uses
US8143397B2 (en) * 2006-02-01 2012-03-27 Medichem S.A. Process for preparing voriconazole, new polymorphic form of intermediate thereof, and uses thereof
AR061889A1 (es) 2006-07-13 2008-10-01 Medichem Sa Proceso mejorado para la preparacion de voriconazol
CN1919846B (zh) * 2006-09-14 2013-01-02 大道隆达（北京）医药科技发展有限公司 伏立康唑及其药用盐、中间体的一种新定向合成制备方法
KR100889937B1 (ko) * 2007-08-06 2009-03-20 한미약품 주식회사 보리코나졸의 제조방법
GB2452049A (en) * 2007-08-21 2009-02-25 Alpharma Aps Process for the preparation of voriconazole
WO2009084029A2 (en) * 2007-12-03 2009-07-09 Neuland Laboratories Ltd Improved process for the preparation of (2r,3s)-2-(2,4- difluqrophenyl)-3-(5-fluoropyrimidin-4-yl)-1-(1h-1,2,4-triazol-1-yl) butan-2-ol
CN101575330B (zh) * 2008-05-05 2012-10-31 丽珠医药集团股份有限公司 伏立康唑广谱抗真菌药物化合物、其组合物及用途
US20110312977A1 (en) * 2009-02-17 2011-12-22 Glenmark Generics Limited Process for the preparation of voriconazole
KR101109215B1 (ko) 2009-06-17 2012-01-30 보령제약 주식회사 보리코나졸의 신규 중간체 및 이를 이용한 보리코나졸의 제조방법
JP2013516394A (ja) 2009-12-30 2013-05-13 メディケム ソシエダ アノニマ 医薬用途用の１−（１ｈ−１，２，４−トリアゾール−１−イル）ブタン−２−オール誘導体、および前記１−（１ｈ−１，２，４−トリアゾール−１−イル）ブタン−２−オール誘導体を調製するための、実質的に不定の結晶形状を有する１−（１ｈ−１，２，４−トリアゾール−１−イル）ブタン−２−オール誘導体の使用
KR100971371B1 (ko) 2010-02-04 2010-07-20 동국제약 주식회사 신규한 중간체를 이용한 보리코나졸의 제조방법
EP2545039A1 (en) 2010-03-10 2013-01-16 Synthon BV A process for making voriconazole
CN101914091B (zh) * 2010-07-25 2015-05-27 浙江华海药业股份有限公司 一种制备伏立康唑中间体的方法
CN102344441B (zh) * 2010-07-25 2015-05-06 浙江华海药业股份有限公司 一种制备伏立康唑中间体的工艺改进方法
PL2678333T3 (pl) 2011-02-21 2015-08-31 Ranbaxy Laboratories Ltd Ulepszony sposób otrzymywania worykonazolu i jego produktów pośrednich
RU2566262C2 (ru) 2011-06-15 2015-10-20 Синтон Бв Стабилизированная композиция вориконазола
CN102516233B (zh) * 2011-12-09 2014-04-09 北京联本医药化学技术有限公司 生产伏立康唑的方法
GR1007802B (el) * 2012-01-31 2013-01-18 Φαρματεν Αβεε, Μεθοδος για την παρασκευη παραγωγου της βρωμοπυρινιδινης
NZ706764A (en) 2012-10-15 2017-11-24 Pfizer Ireland Pharmaceuticals Process for the preparation of voriconazole and analogues thereof
KR101435741B1 (ko) 2013-01-17 2014-08-29 (주) 에프엔지리서치 신규한 보리코나졸 중간체 및 이를 이용한 보리코나졸의 제조 방법
CN105503834B (zh) * 2015-12-23 2021-03-05 浙江华海药业股份有限公司 一种伏立康唑中间体的合成方法
CN106432198B (zh) 2016-09-08 2022-10-21 浙江华海药业股份有限公司 一种制备伏立康唑拆分中间体的方法
CN106632267B (zh) * 2016-11-09 2019-02-22 中国科学院成都生物研究所 一种伏立康唑的合成方法
SG10202105118WA (en) * 2016-11-28 2021-06-29 Cellix Bio Private Ltd Compositions and methods for the treatment of fungal infections
CN108276310A (zh) * 2017-01-06 2018-07-13 常州齐晖药业有限公司 一种伏立康唑拆分剂(r)-10-樟脑磺酸的回收方法
CN108586433A (zh) * 2017-07-21 2018-09-28 齐鲁工业大学 具有抗菌活性的伏立康唑盐酸盐
CN109705102A (zh) * 2019-02-19 2019-05-03 浙江华海立诚药业有限公司 伏立康唑及其中间体的制备方法
CN110305113A (zh) * 2019-07-05 2019-10-08 镇江市第四人民医院（镇江市妇幼保健院） 一种伏立康唑杂质b的合成方法
CN112442017A (zh) * 2019-08-29 2021-03-05 珠海润都制药股份有限公司 一种采用微通道反应器制备伏立康唑消旋体的方法
CN110724130A (zh) * 2019-11-29 2020-01-24 怀化学院 伏立康唑及其中间体的合成方法
CN111440152B (zh) * 2020-05-18 2022-09-27 浙江诚意药业股份有限公司 一种伏立康唑的制备方法
CN112079819B (zh) * 2020-09-24 2022-06-17 南京易亨制药有限公司 一种改进的伏立康唑消旋体制备方法
CN112645935A (zh) * 2020-12-15 2021-04-13 植恩生物技术股份有限公司 伏立康唑关键中间体的制备方法
CN115724829A (zh) * 2022-12-23 2023-03-03 天津力生制药股份有限公司 一种分离真菌药物中间体杂质的液相色谱制备方法

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB8819308D0 (en) * 1988-08-13 1988-09-14 Pfizer Ltd Triazole antifungal agents
GB9002375D0 (en) 1990-02-02 1990-04-04 Pfizer Ltd Triazole antifungal agents
DE69500091T2 (de) * 1994-02-01 1997-05-15 Ube Industries 4-Phenylamino-Pyrimidin-Derivate, Verfahren zur Herstellung und diese enthaltende Schädlingsbekämpfungsmittel für Landwirtschaft und Gartenbau

Also Published As

Publication number Publication date
NO980441L (no) 1998-03-26
AR003472A1 (es) 1998-08-05
RU2156760C2 (ru) 2000-09-27
DE69631160T2 (de) 2004-07-08
JP3211965B2 (ja) 2001-09-25
CA2228655C (en) 2003-09-09
KR19990036174A (ko) 1999-05-25
CZ296975B6 (cs) 2006-08-16
US6946555B2 (en) 2005-09-20
PE16897A1 (es) 1997-05-21
AU703337B2 (en) 1999-03-25
CN1195346A (zh) 1998-10-07
IL122462A0 (en) 1998-06-15
PL187227B1 (pl) 2004-06-30
IL122462A (en) 2001-10-31
PT871625E (pt) 2004-04-30
TR199800170T1 (xx) 1998-06-22
DK0871625T3 (da) 2004-03-29
HUP9802766A3 (en) 2000-03-28
HUP9802766A2 (hu) 1999-02-01
US6586594B1 (en) 2003-07-01
JP3224532B2 (ja) 2001-10-29
ZA966587B (en) 1998-02-02
NO314938B1 (no) 2003-06-16
AU6740396A (en) 1997-03-05
EG21200A (en) 2001-01-31
HU224339B1 (hu) 2005-08-29
DE69631160D1 (de) 2004-01-29
TW442480B (en) 2001-06-23
EP0871625A1 (en) 1998-10-21
CZ32798A3 (cs) 1999-03-17
EP0871625B1 (en) 2003-12-17
WO1997006160A1 (en) 1997-02-20
CN1076019C (zh) 2001-12-12
HK1014944A1 (en) 1999-10-08
ES2210382T3 (es) 2004-07-01
KR100269048B1 (ko) 2000-10-16
NZ315651A (en) 1999-03-29
JP2001354670A (ja) 2001-12-25
CA2228655A1 (en) 1997-02-20
MY123062A (en) 2006-05-31
NO980441D0 (no) 1998-02-02
ATE256679T1 (de) 2004-01-15
IL131521A0 (en) 2001-01-28
PL324922A1 (en) 1998-06-22
US20030181720A1 (en) 2003-09-25
JP2001026583A (ja) 2001-01-30
IN190817B (es) 2003-08-23
GB9516121D0 (en) 1995-10-04
IL131521A (en) 2001-08-08
JPH10510549A (ja) 1998-10-13
BR9609960A (pt) 1999-02-02

Similar Documents

Publication Publication Date Title
MX9801025A (es) Preparacion de triazoles mediante adicion organometalica a cetonas e intermediarios de los mismos.
CA2132199A1 (en) Depsipeptide derivative, production thereof and use thereof
IL175940A0 (en) Prostaglandin synthesis
EP0605392B1 (en) Process for producing methoxyminoacetamide compounds
US4503074A (en) Halogenated geminal diesters
US5750766A (en) Process for the preparation of arylmalonates
EP1036793A3 (en) A process for preparing 2-alkyl-3-aminothiophene derivative and 3-aminothiophene derivative
DK0873327T3 (da) Fremgangsmåde til fremstilling af 2-chlor-5-chlormethyl-thiazol
IL100353A (en) Preparation of 5-(2, 4-difluorophenyl)-salicylic acid and novel 2,4-difluorophenyl-boronic acid derivatives being intermediates therefor
KR890014481A (ko) β-페녹시니트릴 화합물
US5756815A (en) Process for the preparation arylamalonates
GB9520355D0 (en) Chemical process
NZ233196A (en) Process for preparing glutaric acid derivatives and 2-alkoxycarbonylalkyl cyclohexanone derivatives
US5169993A (en) Cyclohexenol derivatives
ES8304920A1 (es) Un procedimiento para preparar derivados de n-acil-n-hidroxi-a minoacidos.
CO4750712A1 (es) Adicion organometalica a cetonas
SI1631533T1 (sl) Nov postopek za stereoselektivno redukcijo beta - ketoestrov
GB2198726A (en) Acylation of methyl 3-methoxy-(2-pyrrol-1-yl) propenoate
HU900968D0 (en) Algicidal compositions and covering compositions thereof
DK1054872T3 (da) Fremgangsmåde til fremstilling af alkoxytriazolinoner
HU901377D0 (en) Process for preparation of carbamates
IL110646A0 (en) Process for the preparation of azoxycyanide compounds
EP1104424A4 (en) PROCESS FOR THE SYNTHESIS OF CARBAPENEM INTERMEDIATES AND COMPOUNDS PRODUCED
KR870006058A (ko) 6H-이소옥사졸로 [3,4-d]피라졸로 [3,4-b]피리딘 및 이의 제조방법

Legal Events

Date Code Title Description
FG Grant or registration
GB Transfer or rights
PD Change of proprietorship

Owner name: PFIZER IRELAND PHARMACEUTICALS

MM Annulment or lapse due to non-payment of fees