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AR036501A1 - Metodo para la sintesis de hexahidro-furo[2,3-b]furan-3-ol, e intermediarios - Google Patents

Metodo para la sintesis de hexahidro-furo[2,3-b]furan-3-ol, e intermediarios

Info

Publication number
AR036501A1
AR036501A1 ARP020103403A ARP020103403A AR036501A1 AR 036501 A1 AR036501 A1 AR 036501A1 AR P020103403 A ARP020103403 A AR P020103403A AR P020103403 A ARP020103403 A AR P020103403A AR 036501 A1 AR036501 A1 AR 036501A1
Authority
AR
Argentina
Prior art keywords
formula
furo
furan
hexahydro
aralkyl
Prior art date
Application number
ARP020103403A
Other languages
English (en)
Original Assignee
Tibotec Pharm Ltd
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=8180908&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR036501(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Tibotec Pharm Ltd filed Critical Tibotec Pharm Ltd
Publication of AR036501A1 publication Critical patent/AR036501A1/es

Links

Classifications

    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/04—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D307/18—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D307/20—Oxygen atoms
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Furan Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Método para la síntesis de hexahidro-furo[2,3-b]furan-3-ol de la fórmula (4) a partir de un intermediario de la fórmula (1) en la cual cada uno de P1 y P2 representa independientemente un hidrógeno, un grupo protector de hidroxi o juntos pueden formar un grupo protector de diol próximo, que comprende transformar dicho intermediario de la fórmula (1) en un derivado de nitrometano de la fórmula (2) en la cual R1 representa alquilo, arilo o aralquilo, R2 representa hidrógeno o C(=O)OR3, R3 representa un alquilo, arilo, aralquilo o R3, en caso de estar presente, y R1, junto con los átomos a los cuales están unidos, pueden formar un grupo cíclico de 6 a 8 miembros que puede estar optativamente sustituido con alquilo, aralquilo o arilo, seguidamente transformar dicho derivado de nitrometano en un derivado de tetrahidrofurano de la fórmula (3) en la cual OR4 representa un alcoholato, y luego transformar el intermediario de la fórmula (3) en hexahidro-furo[2,3-b]furan-3-ol de la fórmula (4) por medio de una reacción de ciclación intramolecular. El hexahidro-furo[2,3-b]furan-3-ol es una parte farmacológica importante presente en la estructura de los inhibidores de proteasa viral.
ARP020103403A 2001-09-10 2002-09-09 Metodo para la sintesis de hexahidro-furo[2,3-b]furan-3-ol, e intermediarios AR036501A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP01203416 2001-09-10

Publications (1)

Publication Number Publication Date
AR036501A1 true AR036501A1 (es) 2004-09-15

Family

ID=8180908

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP020103403A AR036501A1 (es) 2001-09-10 2002-09-09 Metodo para la sintesis de hexahidro-furo[2,3-b]furan-3-ol, e intermediarios

Country Status (28)

Country Link
US (1) US7126015B2 (es)
EP (1) EP1448567B1 (es)
JP (1) JP4521185B2 (es)
KR (1) KR100894673B1 (es)
CN (2) CN100519561C (es)
AP (1) AP1758A (es)
AR (1) AR036501A1 (es)
AT (1) ATE453648T1 (es)
AU (1) AU2002333809C1 (es)
BR (1) BRPI0212341B8 (es)
CA (1) CA2459168C (es)
CY (1) CY1109974T1 (es)
DE (1) DE60234952D1 (es)
DK (1) DK1448567T3 (es)
EA (1) EA010883B1 (es)
ES (1) ES2338538T3 (es)
HK (1) HK1068887A1 (es)
HR (1) HRP20040320B1 (es)
HU (1) HU229505B1 (es)
IL (2) IL160166A0 (es)
MX (1) MXPA04002247A (es)
NO (1) NO328934B1 (es)
NZ (1) NZ531641A (es)
PL (1) PL224030B1 (es)
PT (1) PT1448567E (es)
SI (1) SI21463B (es)
WO (1) WO2003022853A1 (es)
ZA (1) ZA200401501B (es)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2005533821A (ja) * 2002-06-27 2005-11-10 スミスクライン ビーチャム コーポレーション （３α，３α／β，６α／β）ヘキサヒドロフロ［２，３−ｂ］フラン−３−オールの立体異性体の調製
AU2003275675A1 (en) * 2002-12-27 2004-07-29 Sumitomo Chemical Company, Limited Process for producing hexahydrofurofuranol derivative, intermediate thereof and process for producing the same
RS51073B (sr) 2003-12-23 2010-10-31 Tibotec Pharmaceuticals Ltd. Proces za pripremanje (3r,3as,6ar)-heksahidrofuro│2,3-b│ furan-3-il (1s,2r)-3-││(4-aminofenil) sulfonil│(izobutil) amino │-1-benzil-2-hidroksipropilkarbamata
TWI383975B (zh) * 2004-03-31 2013-02-01 Tibotec Pharm Ltd 製備（３Ｒ，３ａＳ，６ａＲ）六氫-呋喃并〔２，３-ｂ〕呋喃-３-醇之方法
JP5549898B2 (ja) * 2006-03-31 2014-07-16 独立行政法人産業技術総合研究所 ５−ヒドロキシメチル−２−フルフラールの製造法
ES2359949T3 (es) * 2006-11-09 2011-05-30 Tibotec Pharmaceuticals Métodos para preparar hexhidrofuro(2,3-b)furan-3-ol.
CN101024646B (zh) * 2007-02-06 2010-07-14 启东东岳药业有限公司 4-甲氧基呋喃并呋喃-2-酮的纯化方法
DE602008005012D1 (de) 2007-04-27 2011-03-31 Little Island Co Cork Herstellungsverfahren für n-isobutyl-n-(2-hydroxy-rivate
US8592487B2 (en) 2007-10-26 2013-11-26 Concert Pharmaceuticals, Inc. Deuterated darunavir
AR073248A1 (es) 2008-09-01 2010-10-20 Tibotec Pharm Ltd Proceso para la preparacion de (1s, 2r)-3- ((4-aminofenil) sulfonil) ( isobutil) amino)-1- bencil-2- hidroxipropilcarbamato de (3r, 3as,6ar)- hexahidrofuro-(2,3-b) furan-3- ilo (darunavir) y compuestos intermediarios utiles en dicho proceso.
EP2358198A4 (en) * 2008-10-24 2012-11-14 Concert Pharmaceuticals Inc HYDROXYETHYLAMINO SULFONAMIDE DERIVATIVES
US8921415B2 (en) 2009-01-29 2014-12-30 Mapi Pharma Ltd. Polymorphs of darunavir
BR112012009956A2 (pt) 2009-10-30 2015-09-29 Lupin Ltd um novo processo para a preparação de darunavir e etanolato darunavir de tamanho de partícula.
BR112012018862A2 (pt) 2010-01-28 2015-10-13 Mapi Pharma Ltd processo para a preparação de darunavir e intermediários de darunavir
WO2012070057A1 (en) 2010-11-23 2012-05-31 Matrix Laboratories Ltd Process for the preparation of (3r, 3as, 6ar)-hexahydrofuro [2, 3- b] furan-3-ol
US8802724B2 (en) 2010-11-30 2014-08-12 Purdue Research Foundation Processes and intermediates for preparing substituted hexahydrofuro [2,3-b] furans
US9475821B2 (en) 2012-07-24 2016-10-25 Laurus Labs Private Limited Process for preparation of Darunavir
ES2657227T3 (es) * 2012-08-09 2018-03-02 Sumitomo Chemical Company, Limited Método para producir un derivado de hexahidrofurofuranol
CN103864813B (zh) * 2012-12-18 2017-02-22 上海迪赛诺化学制药有限公司 一种合成六氢呋喃并[2,3‑b]呋喃‑3‑醇及其对映体的方法
US10633390B2 (en) * 2015-06-25 2020-04-28 Msn Laboratories Private Limited Process for the preparation of [(1S,2R)-3-[[(4-aminophenyl)sulfonyl] (2-methylpropyl)amino]-2-hydroxy-1-(phenylmethyl)propyl]-carbamic acid (3R,3AS,6AR)hexahydro furo [2,3-B]furan-3-YL ester and its amorphous form
WO2017041228A1 (zh) * 2015-09-08 2017-03-16 浙江九洲药业股份有限公司 六氢呋喃并呋喃醇衍生物的制备方法、其中间体及其制备方法
CN107043385B (zh) * 2016-02-05 2019-07-09 成都博腾药业有限公司 一种制备地瑞那韦中间体的方法
ES2881949T3 (es) 2016-10-27 2021-11-30 Gilead Sciences Inc Forma cristalina de base libre de darunavir
CN106928248B (zh) * 2017-02-04 2019-01-04 青岛科技大学 一种制备(3R,3aS,6aR)六氢呋喃并[2,3-b]呋喃-3-醇的方法
CN110272398B (zh) 2018-03-16 2022-11-29 江苏瑞科医药科技有限公司 六氢呋喃并呋喃醇衍生物的制备方法、其中间体及其制备方法
CN114853774A (zh) * 2022-06-24 2022-08-05 盐城迪赛诺制药有限公司 一种达卢那韦关键中间体的制备方法
CN115557964A (zh) * 2022-10-18 2023-01-03 启东东岳药业有限公司 一种药物化合物的制备方法

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Also Published As

Publication number Publication date
DE60234952D1 (de) 2010-02-11
CA2459168A1 (en) 2003-03-20
EA200400430A1 (ru) 2004-08-26
EP1448567A1 (en) 2004-08-25
AP1758A (en) 2007-07-30
AU2002333809B9 (en) 2008-06-26
WO2003022853A1 (en) 2003-03-20
KR20040029425A (ko) 2004-04-06
EA010883B1 (ru) 2008-12-30
HUP0402140A2 (hu) 2005-02-28
BR0212341A (pt) 2004-07-27
SI21463B (sl) 2011-08-31
HU229505B1 (hu) 2014-01-28
PL224030B1 (pl) 2016-11-30
CA2459168C (en) 2014-01-28
BRPI0212341B1 (pt) 2019-04-02
NO20041434L (no) 2004-06-10
KR100894673B1 (ko) 2009-04-24
CN100519561C (zh) 2009-07-29
PT1448567E (pt) 2010-03-12
HUP0402140A3 (en) 2007-05-29
ZA200401501B (en) 2005-07-27
HK1068887A1 (en) 2005-05-06
US20040249175A1 (en) 2004-12-09
SI21463A (sl) 2004-10-31
EP1448567B1 (en) 2009-12-30
IL160166A0 (en) 2004-07-25
BRPI0212341B8 (pt) 2021-05-25
CN101172980B (zh) 2011-11-16
ATE453648T1 (de) 2010-01-15
HRP20040320B1 (hr) 2012-11-30
MXPA04002247A (es) 2005-09-07
DK1448567T3 (da) 2010-04-26
US7126015B2 (en) 2006-10-24
ES2338538T3 (es) 2010-05-10
PL367817A1 (en) 2005-03-07
HRP20040320A2 (en) 2005-04-30
CN101172980A (zh) 2008-05-07
CN1553915A (zh) 2004-12-08
CY1109974T1 (el) 2014-09-10
IL160166A (en) 2012-05-31
NO328934B1 (no) 2010-06-21
AU2002333809B2 (en) 2008-02-28
NZ531641A (en) 2005-08-26
AP2004002981A0 (en) 2004-03-31
JP4521185B2 (ja) 2010-08-11
AU2002333809C1 (en) 2009-02-05
AU2002333809B8 (en) 2008-07-03
JP2005502707A (ja) 2005-01-27

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