BRPI0605907A2 - processo aperfeiçoado para a preparação de letrozol - Google Patents
processo aperfeiçoado para a preparação de letrozolInfo
- Publication number
- BRPI0605907A2 BRPI0605907A2 BRPI0605907-4A BRPI0605907A BRPI0605907A2 BR PI0605907 A2 BRPI0605907 A2 BR PI0605907A2 BR PI0605907 A BRPI0605907 A BR PI0605907A BR PI0605907 A2 BRPI0605907 A2 BR PI0605907A2
- Authority
- BR
- Brazil
- Prior art keywords
- preparation
- benzonitrile
- letrozole
- improved process
- triazolyl
- Prior art date
Links
Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
PROCESSO APERFEIçOADO PARA A PREPARAçãO DE LETROZOL. A invenção fornece um processo de rendimento elevado para a preparação de letrozol com pureza elevada, sem a necessidade de remoção de impreza de 4-[1-(1,3,4-triazolil)metil] benzonitrila no estágio intermediário. A invenção também fornece um processo para síntese de letrezol em que a formação da impureza 4-[1-(1,3,4-triazolil)metil] benzonitrila durante o primeiro estágio é minimizada. no processo, 4-(halometil)benzonitrila reage com um sal de 1H-1,2,4-triazol, reduzindo a formação da impureza. Preferencialmente, a preparação é realizada como um processo de uma única etapa.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US69721705P | 2005-07-06 | 2005-07-06 | |
PCT/US2006/026980 WO2007100346A1 (en) | 2005-07-06 | 2006-07-06 | Improved process for the preparation of letrozole |
Publications (1)
Publication Number | Publication Date |
---|---|
BRPI0605907A2 true BRPI0605907A2 (pt) | 2009-05-26 |
Family
ID=37431706
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BRPI0605907-4A BRPI0605907A2 (pt) | 2005-07-06 | 2006-07-06 | processo aperfeiçoado para a preparação de letrozol |
Country Status (8)
Country | Link |
---|---|
US (1) | US7705159B2 (pt) |
EP (1) | EP1871750A1 (pt) |
JP (1) | JP2008516005A (pt) |
KR (1) | KR100917698B1 (pt) |
CN (1) | CN101253160A (pt) |
BR (1) | BRPI0605907A2 (pt) |
CA (1) | CA2608904A1 (pt) |
WO (1) | WO2007100346A1 (pt) |
Families Citing this family (16)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2007100346A1 (en) | 2005-07-06 | 2007-09-07 | Sicor, Inc. | Improved process for the preparation of letrozole |
US7465749B2 (en) * | 2005-11-14 | 2008-12-16 | Chemagis, Ltd. | Letrozole purification process |
GB2450268B (en) * | 2006-03-17 | 2011-01-12 | Cipla Ltd | Synthesis of 4-[1-(4-cyano phenyl)-1-(1,2,4-triazol-1-yl)methyl]benzonitrile and 4-[1-(1,2,4-triazol-1-yl)methyl]benzonitrile intermediate |
EP2026797A2 (en) | 2006-05-25 | 2009-02-25 | Synta Pharmaceuticals Corporation | Method for treating non-hodgkin's lymphoma |
ATE547409T1 (de) * | 2007-11-28 | 2012-03-15 | Fresenius Kabi Oncology Ltd | Verbessertes verfahren zur herstellung von letrozol und zwischenprodukten davon |
WO2011000396A1 (en) * | 2009-07-02 | 2011-01-06 | Synthon B.V. | Purification of letrozole intermediate |
EP2560640A1 (en) | 2010-04-19 | 2013-02-27 | Synta Pharmaceuticals Corp. | Cancer therapy using a combination of a hsp90 inhibitory compounds and a egfr inhibitor |
US9150524B2 (en) | 2010-08-27 | 2015-10-06 | Generics [Uk] Limited | Pure intermediate |
JP2014532712A (ja) | 2011-11-02 | 2014-12-08 | シンタ ファーマシューティカルズ コーポレーション | トポイソメラーゼi阻害剤とhsp90阻害剤の組合せを使用する癌療法 |
US20140286902A1 (en) | 2011-11-02 | 2014-09-25 | Synta Pharmaceuticals Corp. | Combination therapy of hsp90 inhibitors with platinum-containing agents |
EP2780010A1 (en) | 2011-11-14 | 2014-09-24 | Synta Pharmaceuticals Corp. | Combination therapy of hsp90 inhibitors with braf inhibitors |
CN103242198A (zh) * | 2013-04-25 | 2013-08-14 | 哈药集团制药总厂 | 一种来曲唑杂质的制备方法 |
CN103664810B (zh) * | 2013-12-11 | 2016-09-14 | 深圳劲创生物技术有限公司 | 一种合成来曲唑的工艺 |
MX2020002649A (es) | 2017-09-11 | 2020-09-25 | Atossa Therapeutics Inc | Metodos para hacer y usar endoxifeno. |
CN109721558A (zh) * | 2017-10-27 | 2019-05-07 | 中国医学科学院药物研究所 | 来曲唑晶iii型固体物质及制备方法和其药物组合物与用途 |
CN109721557A (zh) * | 2017-10-27 | 2019-05-07 | 中国医学科学院药物研究所 | 来曲唑晶ii型固体物质及制备方法和其药物组合物与用途 |
Family Cites Families (19)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4978672A (en) * | 1986-03-07 | 1990-12-18 | Ciba-Geigy Corporation | Alpha-heterocyclc substituted tolunitriles |
US5352795A (en) * | 1986-03-07 | 1994-10-04 | Ciba-Geigy Corporation | Alpha-heterocycle substituted tolunitriles |
US4749713A (en) * | 1986-03-07 | 1988-06-07 | Ciba-Geigy Corporation | Alpha-heterocycle substituted tolunitriles |
DE3926365A1 (de) * | 1989-08-04 | 1991-02-07 | Schering Ag | Cycloalkylenazole, verfahren zu deren herstellung, pharmazeutische praeparate, die diese enthalten sowie ihre verwendung zur herstellung von arzneimitteln |
EP1594850A2 (en) | 2003-02-06 | 2005-11-16 | Sun Pharmaceuticals Industries Ltd. | Regiospecific process for the preparation of 4- 1- (4-cyanophenyl)-1-(1,2,4-triazol-1-yl)methyl]benzonitrile |
AU2003282380A1 (en) * | 2003-11-14 | 2004-06-06 | ADIBHATLA, KALI,SATYA, Bhujanga,rao | A method for the separation of the letrozole precursor 4-1-(1,2,4-triazolyl) methyl benzonitrile from its 1,3,4-triazolyl isomer |
US20050209294A1 (en) * | 2004-03-17 | 2005-09-22 | Wadhwa Lalit K | Process for producing 4-(1H-1,2,4-triazol-1-ylmethyl)benzonitrile |
WO2007100346A1 (en) | 2005-07-06 | 2007-09-07 | Sicor, Inc. | Improved process for the preparation of letrozole |
WO2007039912A1 (en) | 2005-10-05 | 2007-04-12 | Usv Limited | A one pot process for the preparation of 4-[1-cyanophenyl)-1-(1,2,4-triazol-1-yl)methyl]benzonitrile |
US20100190997A1 (en) | 2005-10-20 | 2010-07-29 | Hussain Haider | Process for the Preparation of Letrozole |
US20070100149A1 (en) | 2005-11-02 | 2007-05-03 | Palle Venkata Raghavendra A | Process for preparing letrozole |
US7538230B2 (en) | 2005-11-14 | 2009-05-26 | Chemagis Ltd. | Letrozole production process |
US7465749B2 (en) | 2005-11-14 | 2008-12-16 | Chemagis, Ltd. | Letrozole purification process |
WO2007074474A1 (en) | 2005-12-27 | 2007-07-05 | Dabur Pharma Limited | Novel intermediates for preparation of letrozole |
WO2007090464A1 (en) | 2006-02-08 | 2007-08-16 | Solmag S.P.A. | Process for preparing letrozole |
GB2450268B (en) | 2006-03-17 | 2011-01-12 | Cipla Ltd | Synthesis of 4-[1-(4-cyano phenyl)-1-(1,2,4-triazol-1-yl)methyl]benzonitrile and 4-[1-(1,2,4-triazol-1-yl)methyl]benzonitrile intermediate |
WO2007128561A1 (en) | 2006-05-04 | 2007-11-15 | Synthon B.V. | Crystalline forms of letrozole and processes for making them |
WO2007144896A1 (en) | 2006-06-13 | 2007-12-21 | Natco Pharma Limited | A method of manufacture of letrozole |
EP2155698A1 (en) | 2007-01-22 | 2010-02-24 | Natco Pharma Limited | Novel thermodynamically stable polymorphic form-l of letrozole |
-
2006
- 2006-07-06 WO PCT/US2006/026980 patent/WO2007100346A1/en active Application Filing
- 2006-07-06 EP EP06786958A patent/EP1871750A1/en not_active Withdrawn
- 2006-07-06 CA CA002608904A patent/CA2608904A1/en not_active Abandoned
- 2006-07-06 CN CNA2006800237650A patent/CN101253160A/zh active Pending
- 2006-07-06 BR BRPI0605907-4A patent/BRPI0605907A2/pt not_active IP Right Cessation
- 2006-07-06 KR KR1020077007718A patent/KR100917698B1/ko not_active IP Right Cessation
- 2006-07-06 US US11/482,228 patent/US7705159B2/en not_active Expired - Fee Related
- 2006-07-06 JP JP2008503298A patent/JP2008516005A/ja active Pending
Also Published As
Publication number | Publication date |
---|---|
CA2608904A1 (en) | 2007-09-07 |
EP1871750A1 (en) | 2008-01-02 |
WO2007100346A1 (en) | 2007-09-07 |
KR20070105299A (ko) | 2007-10-30 |
KR100917698B1 (ko) | 2009-09-21 |
CN101253160A (zh) | 2008-08-27 |
JP2008516005A (ja) | 2008-05-15 |
US7705159B2 (en) | 2010-04-27 |
US20070066831A1 (en) | 2007-03-22 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
B08F | Application fees: application dismissed [chapter 8.6 patent gazette] |
Free format text: REFERENTE AS 3A, 4A, 5A E 6A ANUIDADES. |
|
B08K | Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette] |
Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2161 DE 05/06/2012. |