BRPI0417272A - processo para a preparação de (3r, 3as, 6ar)-hexahidrofuro [2,3-b] furan-3-3il (1s, 2r)-3-[[(4-aminofenil) sulfonil] (isobutil) amino]-1-benzil-2-hidroxipropilcarbamato - Google Patents

processo para a preparação de (3r, 3as, 6ar)-hexahidrofuro [2,3-b] furan-3-3il (1s, 2r)-3-[[(4-aminofenil) sulfonil] (isobutil) amino]-1-benzil-2-hidroxipropilcarbamato

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Publication number
BRPI0417272A
BRPI0417272A BRPI0417272-8A BRPI0417272A BRPI0417272A BR PI0417272 A BRPI0417272 A BR PI0417272A BR PI0417272 A BRPI0417272 A BR PI0417272A BR PI0417272 A BRPI0417272 A BR PI0417272A
Authority
BR
Brazil
Prior art keywords
amino
isobutyl
hexahydrofuro
aminophenyl
furan
Prior art date
Application number
BRPI0417272-8A
Other languages
English (en)
Inventor
Nicolaas Martha Feli Goyvaerts
Piet Tom Bert Paul Wigerinck
Hartmut Burghard Zinser
Birgit M Ebert
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
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Application filed by Tibotec Pharm Ltd filed Critical Tibotec Pharm Ltd
Publication of BRPI0417272A publication Critical patent/BRPI0417272A/pt
Publication of BRPI0417272B1 publication Critical patent/BRPI0417272B1/pt
Publication of BRPI0417272B8 publication Critical patent/BRPI0417272B8/pt

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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Furan Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

"PROCESSO PARA A PREPARAçãO DE (3R,3AS,6AR)-HEXAHIDROFURO ¢2,3-B! FURAN-3-IL (1S,2R)-3-¢¢(4AMINOFENIL) SULFONIL! (ISOBUTIL) AMINO!-1-BENZIL-2HIDROXIPROPILCARBAMATO". A presente invenção refere-se a um processo para a preparação de (3R,3aS,6aR)hexahidrofuro ¢2,3-b! furan-3-il (1S,2R)-3-¢¢(4-aminofenil) sulfonil! (isobutil) amino!-1-benzil-2-hidroxipropilcarbamato bem como intermediários para uso em ditos processos. Mais em particular, a invenção relaciona-se a processos para a preparação de (3R,3aS,6aR)hexahidrofuro ¢2,3b! furan-3-il (1S,2R)-3-¢¢(4-aminofenil) sulfonil! (isobutil) amino !-1-benzil-2hidroxipropilcarbamato o qual faz uso do intermediário 4-amino-N¢(2R,3S)-3amino-2-hidróxi-4-fenilbutil!-N-isobutil)benzeno sulfonamida, e os quais são processos amenáveis a escala industrial. (3R,3aS,6aR)hexahidrofuro ¢2,3-b! furan-3-il (1S,2R)-3-¢¢(4-aminofenil) sulfonil! (isobutil) amino!-1-benzil-2hidroxipropilcarbamato é particularmente útil como inibidor de HIV-protease.
BRPI0417272A 2003-12-23 2004-12-23 processo para a preparação de (3r, 3as, 6ar)-hexahidrofuro [2,3-b] furan-3-il (1s, 2r)-3-[[(4-aminofenil) sulfonil] (isobutil) amino]-1-benzil-2-hidroxipropilcarbamato BRPI0417272B8 (pt)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP03104949 2003-12-23
EP031049497 2003-12-23
US56818304P 2004-05-04 2004-05-04
US60/568,183 2004-05-04
PCT/EP2004/053692 WO2005063770A1 (en) 2003-12-23 2004-12-23 Process for the preparation of (3r,3as,6ar)-hexahydrofuro [2,3-b] furan-3-yl (1s,2r)-3-[[(4-aminophenyl) sulfonyl] (isobutyl) amino]-1-benzyl-2-hydroxypropylcarbamate

Publications (3)

Publication Number Publication Date
BRPI0417272A true BRPI0417272A (pt) 2007-03-27
BRPI0417272B1 BRPI0417272B1 (pt) 2020-08-18
BRPI0417272B8 BRPI0417272B8 (pt) 2021-05-25

Family

ID=34740665

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0417272A BRPI0417272B8 (pt) 2003-12-23 2004-12-23 processo para a preparação de (3r, 3as, 6ar)-hexahidrofuro [2,3-b] furan-3-il (1s, 2r)-3-[[(4-aminofenil) sulfonil] (isobutil) amino]-1-benzil-2-hidroxipropilcarbamato

Country Status (21)

Country Link
EP (1) EP1725566B1 (pt)
KR (1) KR101192859B1 (pt)
CN (1) CN1898248B (pt)
AT (1) ATE433982T1 (pt)
AU (1) AU2004309122B2 (pt)
BR (1) BRPI0417272B8 (pt)
CA (1) CA2549460C (pt)
CY (1) CY1109379T1 (pt)
DE (1) DE602004021640D1 (pt)
DK (1) DK1725566T3 (pt)
ES (1) ES2328701T3 (pt)
HR (1) HRP20090488T1 (pt)
IL (1) IL174960A (pt)
MX (1) MXPA06007211A (pt)
NO (1) NO337636B1 (pt)
PL (1) PL1725566T3 (pt)
PT (1) PT1725566E (pt)
RU (1) RU2376308C2 (pt)
SI (1) SI1725566T1 (pt)
WO (1) WO2005063770A1 (pt)
ZA (1) ZA200605163B (pt)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI432438B (zh) 2005-11-28 2014-04-01 Tibotec Pharm Ltd 作為ｈｉｖ蛋白酶抑制劑之經取代的胺基苯基磺醯胺化合物及衍生物
RS51675B (sr) * 2006-11-09 2011-10-31 Tibotec Pharmaceuticals Metode za dobivanje heksahidrofuro[2,3-b]furan-3-ola
WO2008132154A1 (en) 2007-04-27 2008-11-06 Tibotec Pharmaceuticals Ltd. Methods for the preparation of n-isobutyl-n-(2-hydroxy-3-amino-4-phenylbutyl)-p-nitrobenzenesulfonylamide derivatives
US8592487B2 (en) 2007-10-26 2013-11-26 Concert Pharmaceuticals, Inc. Deuterated darunavir
WO2009055006A1 (en) * 2007-10-26 2009-04-30 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.
US8921415B2 (en) 2009-01-29 2014-12-30 Mapi Pharma Ltd. Polymorphs of darunavir
DK2426124T3 (da) * 2009-05-13 2013-09-30 Meiji Seika Pharma Co Ltd Fremgangsmåde til fremstilling af pyripyropene derivater
CA2776807C (en) 2009-09-17 2018-10-16 Mylan Laboratories Limited An improved process for the preparation of darunavir
WO2011083287A2 (en) 2010-01-05 2011-07-14 Cipla Limited Darunavir polymorph and process for preparation thereof
PL2528923T3 (pl) 2010-01-28 2015-01-30 Mapi Pharma Ltd Sposób wytwarzania darunawiru i pochodnych darunawiru
CN102584844B (zh) * 2011-01-11 2016-04-13 浙江九洲药业股份有限公司 一种达芦那韦晶型及其制备方法
EP3795572B1 (en) 2012-07-24 2023-11-15 Laurus Labs Limited Darunavir propionate solvate
CN103893178B (zh) * 2014-03-19 2016-06-01 中山大学 苯-磺酰胺类化合物在制备抗hiv-1病毒药物中的应用
US20160075643A1 (en) * 2014-09-16 2016-03-17 Zcl Chemicals Limited Novel process to prepare intermediates of hiv-protease inhibitors thereof
WO2016207907A1 (en) * 2015-06-25 2016-12-29 Msn Laboratories Private Limited Process for the preparation of [(1 s,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
EP3532478B1 (en) 2016-10-27 2021-05-26 Gilead Sciences, Inc. Crystalline form of darunavir free base
DK3541819T3 (da) * 2016-11-17 2021-02-22 Janssen Sciences Ireland Unlimited Co Forenklet procedure til fremstilling af darunavir
CN114685322B (zh) * 2020-12-30 2023-08-25 上海飞腾医药科技有限公司 一种抗hiv类药物中间体晶体的生长方法和所得晶体及其应用
CN113896658A (zh) * 2021-09-24 2022-01-07 上药康丽（常州）药业有限公司 一种利用微通道反应器合成地瑞那韦中间体的方法

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DE69637380T2 (de) 1995-01-20 2009-09-17 G.D. Searle Llc, Chicago Bis-sulfonamid-hydroxyethylamino-derivate als inhibitoren retroviraler proteasen
EP0754669B1 (en) 1995-02-03 2001-10-31 Kaneka Corporation Processes for producing alpha-halo ketones, alpha-halohydrins and epoxides
US5756533A (en) 1995-03-10 1998-05-26 G.D. Searle & Co. Amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
US6150556A (en) 1995-03-10 2000-11-21 G. D. Dearle & Co. Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
US5705500A (en) 1995-03-10 1998-01-06 G.D. Searle & Co. Sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors
CN1149223C (zh) 1995-03-10 2004-05-12 G·D·瑟尔公司 杂环羰基氨基酸羟乙氨基磺酰胺逆转录病毒蛋白酶抑制剂
GB9805898D0 (en) * 1998-03-20 1998-05-13 Glaxo Group Ltd Process for the sythesis of hiv protease inhibitors
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EP1466896A4 (en) * 2001-12-28 2005-01-26 Ajinomoto Kk PROCESS FOR PRODUCING A CRYSTAL OF A BENZENESULFONAMIDE DERIVATIVE, AND A NEW CRYSTAL OF AN INTERMEDIATE PRODUCT OF SAID DERIVATIVE AND METHOD FOR PRODUCING THE SAME

Also Published As

Publication number Publication date
BRPI0417272B1 (pt) 2020-08-18
BRPI0417272B8 (pt) 2021-05-25
PT1725566E (pt) 2009-09-16
NO20063401L (no) 2006-07-21
WO2005063770A1 (en) 2005-07-14
CA2549460C (en) 2014-08-05
EP1725566A1 (en) 2006-11-29
PL1725566T3 (pl) 2009-11-30
RU2006126670A (ru) 2008-01-27
IL174960A (en) 2011-06-30
DE602004021640D1 (de) 2009-07-30
ES2328701T3 (es) 2009-11-17
CA2549460A1 (en) 2005-07-14
AU2004309122A1 (en) 2005-07-14
RU2376308C2 (ru) 2009-12-20
CN1898248A (zh) 2007-01-17
CY1109379T1 (el) 2014-07-02
AU2004309122B2 (en) 2011-07-21
ZA200605163B (en) 2007-12-27
MXPA06007211A (es) 2006-08-18
DK1725566T3 (da) 2009-10-05
IL174960A0 (en) 2006-08-20
CN1898248B (zh) 2011-08-17
HRP20090488T1 (hr) 2009-10-31
KR20060123740A (ko) 2006-12-04
EP1725566B1 (en) 2009-06-17
NO337636B1 (no) 2016-05-23
KR101192859B1 (ko) 2012-10-19
ATE433982T1 (de) 2009-07-15
SI1725566T1 (sl) 2009-12-31

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Legal Events

Date Code Title Description
B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B15K Others concerning applications: alteration of classification

Free format text: PARA INT.CL: C07D 493/04, A61P 31/00

Ipc: C07D 493/04 (2011.01)

B25D Requested change of name of applicant approved

Owner name: TIBOTEC PHARMACEUTICALS (IE)

B25D Requested change of name of applicant approved

Owner name: JANSSEN R AND D IRELAND (IE)

B25A Requested transfer of rights approved

Owner name: JANSSEN SCIENCES IRELAND UC (IE)

B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]

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