NZ607428A - Pure intermediate for preparing letrozole - Google Patents
Pure intermediate for preparing letrozoleInfo
- Publication number
- NZ607428A NZ607428A NZ607428A NZ60742811A NZ607428A NZ 607428 A NZ607428 A NZ 607428A NZ 607428 A NZ607428 A NZ 607428A NZ 60742811 A NZ60742811 A NZ 60742811A NZ 607428 A NZ607428 A NZ 607428A
- Authority
- NZ
- New Zealand
- Prior art keywords
- triazol
- benzonitrile
- methyl
- iii
- salt
- Prior art date
Links
- HPJKCIUCZWXJDR-UHFFFAOYSA-N letrozole Chemical compound C1=CC(C#N)=CC=C1C(N1N=CN=C1)C1=CC=C(C#N)C=C1 HPJKCIUCZWXJDR-UHFFFAOYSA-N 0.000 title abstract 4
- 229960003881 letrozole Drugs 0.000 title abstract 3
- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 abstract 9
- 150000003839 salts Chemical class 0.000 abstract 7
- JFDZBHWFFUWGJE-UHFFFAOYSA-N benzonitrile Chemical compound N#CC1=CC=CC=C1 JFDZBHWFFUWGJE-UHFFFAOYSA-N 0.000 abstract 6
- HQLYWHSJALKYOV-UHFFFAOYSA-N 4-(1,2,4-triazol-1-ylmethyl)benzonitrile Chemical compound C1=CC(C#N)=CC=C1CN1N=CN=C1 HQLYWHSJALKYOV-UHFFFAOYSA-N 0.000 abstract 4
- 238000000034 method Methods 0.000 abstract 3
- 235000006408 oxalic acid Nutrition 0.000 abstract 3
- 125000003626 1,2,4-triazol-1-yl group Chemical group [*]N1N=C([H])N=C1[H] 0.000 abstract 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 2
- 238000002360 preparation method Methods 0.000 abstract 2
- AEKVBBNGWBBYLL-UHFFFAOYSA-N 4-fluorobenzonitrile Chemical compound FC1=CC=C(C#N)C=C1 AEKVBBNGWBBYLL-UHFFFAOYSA-N 0.000 abstract 1
- 238000006243 chemical reaction Methods 0.000 abstract 1
- 238000000746 purification Methods 0.000 abstract 1
Classifications
-
- 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
-
- 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
- A61K31/4196—1,2,4-Triazoles
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN2395MU2010 | 2010-08-27 | ||
| PCT/GB2011/051611 WO2012025762A2 (en) | 2010-08-27 | 2011-08-26 | Pure intermediate |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| NZ607428A true NZ607428A (en) | 2015-10-30 |
Family
ID=44653355
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NZ607428A NZ607428A (en) | 2010-08-27 | 2011-08-26 | Pure intermediate for preparing letrozole |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US9150524B2 (enExample) |
| EP (1) | EP2609087A2 (enExample) |
| JP (1) | JP5958863B2 (enExample) |
| CN (1) | CN103298795A (enExample) |
| CA (1) | CA2809086A1 (enExample) |
| NZ (1) | NZ607428A (enExample) |
| WO (1) | WO2012025762A2 (enExample) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| CN117924195A (zh) * | 2023-08-23 | 2024-04-26 | 中科帆凯(大连)新材料有限公司 | 一种制备纯的来曲唑中间体的方法 |
| CN117285477A (zh) * | 2023-09-04 | 2023-12-26 | 河南康达制药有限公司 | 一种来曲唑的合成工艺及其装置 |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4978672A (en) | 1986-03-07 | 1990-12-18 | Ciba-Geigy Corporation | Alpha-heterocyclc substituted tolunitriles |
| US4749713A (en) | 1986-03-07 | 1988-06-07 | Ciba-Geigy Corporation | Alpha-heterocycle substituted tolunitriles |
| CN1325482C (zh) | 2001-12-11 | 2007-07-11 | 埃默里大学 | 双(氰基苯基)甲基－三唑在预防乳腺癌中的用途 |
| WO2004076409A2 (en) * | 2003-02-06 | 2004-09-10 | Sun Pharmaceutical Industries Limited | 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 |
| CN100560573C (zh) * | 2004-09-28 | 2009-11-18 | 北京德众万全医药科技有限公司 | 一种高纯度来曲唑的制备方法 |
| CA2608904A1 (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 |
| WO2007054964A2 (en) | 2005-10-20 | 2007-05-18 | Cadila Healthcare Limited | Process for the preparation of letrozole |
| WO2007090464A1 (en) | 2006-02-08 | 2007-08-16 | Solmag S.P.A. | Process for preparing letrozole |
| US8003804B2 (en) | 2006-03-17 | 2011-08-23 | Cipla Limited | Synthesis of 4-[1-(4-cyano phenyl)-(1,2,4-triazol-1-yl)methyl] benzonitrile and 4-[1-(1H-1,2,4-triazol-1-yl)methylene benzonitrile intermediate |
| WO2007144896A1 (en) | 2006-06-13 | 2007-12-21 | Natco Pharma Limited | A method of manufacture of letrozole |
| CN101033214B (zh) * | 2006-07-06 | 2011-05-18 | 上海复旦复华药业有限公司 | 来曲唑的制备方法 |
| US8198460B2 (en) | 2007-11-28 | 2012-06-12 | Fresenius Kabi Oncology Ltd. | Process for preparation of letrozole and its intermediates |
| WO2010146391A1 (en) | 2009-06-15 | 2010-12-23 | Generics [Uk] Limited | Regioselective synthesis of letrozole |
| WO2011000396A1 (en) | 2009-07-02 | 2011-01-06 | Synthon B.V. | Purification of letrozole intermediate |
-
2011
- 2011-08-26 WO PCT/GB2011/051611 patent/WO2012025762A2/en not_active Ceased
- 2011-08-26 CN CN2011800500261A patent/CN103298795A/zh active Pending
- 2011-08-26 NZ NZ607428A patent/NZ607428A/en not_active IP Right Cessation
- 2011-08-26 US US13/818,815 patent/US9150524B2/en active Active
- 2011-08-26 CA CA2809086A patent/CA2809086A1/en not_active Abandoned
- 2011-08-26 JP JP2013525364A patent/JP5958863B2/ja not_active Expired - Fee Related
- 2011-08-26 EP EP11757922.7A patent/EP2609087A2/en not_active Withdrawn
Also Published As
| Publication number | Publication date |
|---|---|
| JP5958863B2 (ja) | 2016-08-02 |
| CA2809086A1 (en) | 2012-03-01 |
| CN103298795A (zh) | 2013-09-11 |
| AU2011294906B2 (en) | 2016-05-19 |
| EP2609087A2 (en) | 2013-07-03 |
| WO2012025762A2 (en) | 2012-03-01 |
| US20130203826A1 (en) | 2013-08-08 |
| JP2013536217A (ja) | 2013-09-19 |
| AU2011294906A1 (en) | 2013-03-14 |
| AU2011294906A8 (en) | 2016-05-26 |
| WO2012025762A3 (en) | 2012-05-03 |
| US9150524B2 (en) | 2015-10-06 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PSEA | Patent sealed | ||
| RENW | Renewal (renewal fees accepted) |
Free format text: PATENT RENEWED FOR 3 YEARS UNTIL 26 AUG 2018 BY SPRUSON + FERGUSON Effective date: 20160309 |
|
| RENW | Renewal (renewal fees accepted) |
Free format text: PATENT RENEWED FOR 1 YEAR UNTIL 26 AUG 2019 BY RENEWALS TEAM Effective date: 20180614 |
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| RENW | Renewal (renewal fees accepted) |
Free format text: PATENT RENEWED FOR 1 YEAR UNTIL 26 AUG 2020 BY RENEWALS TEAM Effective date: 20190819 |
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| RENW | Renewal (renewal fees accepted) |
Free format text: PATENT RENEWED FOR 1 YEAR UNTIL 26 AUG 2021 BY ENVOY Effective date: 20200822 |
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| LAPS | Patent lapsed |