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
AR058238A1 (es) * 2005-11-28 2008-01-23 Tibotec Pharm Ltd Compuestos y derivados de aminofenilsulfonamida sustituida como inhibidores de proteasa del vih
SI2089371T1 (sl) 2006-11-09 2011-05-31 Tibotec Pharm Ltd Postopki za pripravo heksahidrofuro(2,3-b)furan-3-ola
AU2008244306A1 (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
CA2703591C (en) * 2007-10-26 2013-05-07 Concert Pharmaceuticals, Inc. Deuterated darunavir
TWI482775B (zh) * 2008-09-01 2015-05-01 Tibotec Pharm Ltd 用於製備（３ｒ，３ａｓ，６ａｒ）－六氫呋喃并〔２，３－ｂ〕呋喃－３－基（１ｓ，２ｒ）－３－〔〔（４－胺基苯基）磺醯基〕（異丁基）胺基〕－１－苯甲基－２－羥基丙基胺基甲酸酯之方法
US8921415B2 (en) 2009-01-29 2014-12-30 Mapi Pharma Ltd. Polymorphs of darunavir
MX2011011414A (es) * 2009-05-13 2011-12-06 Meiji Seika Pharma Co Ltd Proceso para producir derivados de piripiropeno.
EP2477992B1 (en) 2009-09-17 2016-12-14 Mylan Laboratories Limited Processes for the preparation of darunavir and the amorphous form thereof
JP2013516397A (ja) 2010-01-05 2013-05-13 シプラ・リミテッド ダルナビルの多形及びその製造方法
ES2516916T3 (es) 2010-01-28 2014-10-31 Mapi Pharma Limited Procedimiento para la preparación de darunavir e intermedios de darunavir
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
ES2881949T3 (es) 2016-10-27 2021-11-30 Gilead Sciences Inc Forma cristalina de base libre de darunavir
PL3541819T3 (pl) * 2016-11-17 2021-06-14 Janssen Sciences Ireland Unlimited Company Uproszczona procedura wytwarzania darunawiru
CN118026896A (zh) * 2020-12-30 2024-05-14 上海飞腾医药科技有限公司 抗hiv类药物中间体晶体的生长方法和所得晶体
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

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4014220B2 (ja) 1995-01-20 2007-11-28 ジー．ディー．サール アンド カンパニー ビス−スルホンアミドヒドロキシエチルアミノ レトロ ウイルスプロテアーゼインヒビター
JP3665343B2 (ja) 1995-02-03 2005-06-29 株式会社カネカ α−ハロケトン、α−ハロヒドリン及びエポキシドの製造法
US5756533A (en) 1995-03-10 1998-05-26 G.D. Searle & Co. Amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
RU2174519C2 (ru) 1995-03-10 2001-10-10 Джи. Ди. Сирл Энд Ко. Гидроксиэтиламино сульфонамиды гетероциклокарбонил аминокислоты, ингибирующие ретровирусную протеазу
US6150556A (en) 1995-03-10 2000-11-21 G. D. Dearle & Co. Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
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ATE334121T1 (de) 1999-01-29 2006-08-15 Kaneka Corp Verfahren zur herstellung von threo-1,2-epoxy-3- amino-4-phenylbutan-derivaten
US6764545B2 (en) 2000-12-12 2004-07-20 Ajinomoto Co., Inc. Production method of epoxide crystal
AR035970A1 (es) 2001-05-11 2004-07-28 Tibotec Pharm Ltd 2-amino-benzoxazol sulfonamidas inhibidoras de amplio espectro de la hiv proteasa, composicion farmaceutica, metodo "in vitro" para inhibir la replicacion retroviral, y utilizacion de estos compuestos en la manufactura de medicamentos
WO2003057665A1 (fr) * 2001-12-28 2003-07-17 Ajinomoto Co., Inc. Procede de production d'un cristal d'un derive de benzenesulfonamide, et nouveau cristal d'un produit intermediaire de ce derive et son procede de production

Also Published As

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

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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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B06U Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette]
B06I Publication of requirement cancelled [chapter 6.9 patent gazette]

Free format text: ANULADA A PUBLICACAO CODIGO 6.21 NA RPI NO 2552 DE 03/12/2019 POR TER SIDO INDEVIDA.

B06A Patent application procedure suspended [chapter 6.1 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]
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