ATE292116T1 - Verfahren zur herstellung von donepezilderivaten - Google Patents
Verfahren zur herstellung von donepezilderivatenInfo
- Publication number
- ATE292116T1 ATE292116T1 AT99900320T AT99900320T ATE292116T1 AT E292116 T1 ATE292116 T1 AT E292116T1 AT 99900320 T AT99900320 T AT 99900320T AT 99900320 T AT99900320 T AT 99900320T AT E292116 T1 ATE292116 T1 AT E292116T1
- Authority
- AT
- Austria
- Prior art keywords
- reaction
- derivative
- salt
- pyridyl
- methyl
- Prior art date
Links
- ADEBPBSSDYVVLD-UHFFFAOYSA-N donepezil Chemical class O=C1C=2C=C(OC)C(OC)=CC=2CC1CC(CC1)CCN1CC1=CC=CC=C1 ADEBPBSSDYVVLD-UHFFFAOYSA-N 0.000 title abstract 2
- 238000004519 manufacturing process Methods 0.000 title abstract 2
- 238000006243 chemical reaction Methods 0.000 abstract 3
- -1 carbonate ester Chemical class 0.000 abstract 2
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- SQGMRMOPTFCLKQ-UHFFFAOYSA-N 2-(pyridin-4-ylmethyl)-2,3-dihydroinden-1-one Chemical class C1C2=CC=CC=C2C(=O)C1CC1=CC=NC=C1 SQGMRMOPTFCLKQ-UHFFFAOYSA-N 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 238000006114 decarboxylation reaction Methods 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- QNXSIUBBGPHDDE-UHFFFAOYSA-N indan-1-one Chemical class C1=CC=C2C(=O)CCC2=C1 QNXSIUBBGPHDDE-UHFFFAOYSA-N 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 230000000144 pharmacologic effect Effects 0.000 abstract 1
- 150000003242 quaternary ammonium salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/44—Radicals substituted by doubly-bound oxygen, sulfur, or nitrogen atoms, or by two such atoms singly-bound to the same carbon atom
- C07D213/46—Oxygen atoms
- C07D213/50—Ketonic radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D211/30—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom
- C07D211/32—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom by oxygen atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pyridine Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP690898 | 1998-01-16 | ||
| PCT/JP1999/000111 WO1999036405A1 (en) | 1998-01-16 | 1999-01-14 | Process for production of donepezil derivative |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ATE292116T1 true ATE292116T1 (de) | 2005-04-15 |
Family
ID=11651348
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AT99900320T ATE292116T1 (de) | 1998-01-16 | 1999-01-14 | Verfahren zur herstellung von donepezilderivaten |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US6252081B1 (de) |
| EP (1) | EP1047674B1 (de) |
| AT (1) | ATE292116T1 (de) |
| CA (1) | CA2316360C (de) |
| DE (1) | DE69924467T2 (de) |
| ES (1) | ES2237078T3 (de) |
| WO (1) | WO1999036405A1 (de) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20060183776A9 (en) * | 2000-03-03 | 2006-08-17 | Eisai Co., Ltd. | Liquid dosage formulations of donepezil |
| WO2001066114A1 (en) | 2000-03-03 | 2001-09-13 | Eisai Co., Ltd. | Novel methods using cholinesterase inhibitors |
| US6706741B2 (en) * | 2000-04-13 | 2004-03-16 | Eisai Co., Ltd. | Acetylcholinesterase inhibitors containing 1-benzyl-pyridinium salts |
| IL150982A (en) * | 2002-07-30 | 2007-02-11 | Ori Lerman | Process for making Donafzil |
| US6953856B2 (en) * | 2003-02-12 | 2005-10-11 | Usv, Limited | Process for the preparation of 1-benzyl-4-(5,6-dimethoxy-1-indanon)-2-yl) methyl piperidine hydrochloride (Donepezil HCI) |
| US6649765B1 (en) | 2003-02-12 | 2003-11-18 | Usv Limited, Bsd Marg. | Process for the preparation of 1-benzyl-4(5,6-dimethoxy-1-indanon)-2-yl) methyl piperidine hydrochloride (Donepezil HCL) |
| EP1608371A1 (de) * | 2003-03-21 | 2005-12-28 | Ranbaxy Laboratories, Ltd. | Verfahren zur herstellung von donepezil und derivaten |
| WO2004099142A1 (en) * | 2003-05-05 | 2004-11-18 | Ranbaxy Laboratories Limited | Hydrobromide salt of benzyl-piperidylmethyl-indanone and its polymorphs |
| EP1654230A1 (de) | 2003-07-01 | 2006-05-10 | Hetero Drugs Limited | Herstellung von zwischenprodukten für acetylcholinesteraseinhibitoren |
| CN1280273C (zh) * | 2003-11-05 | 2006-10-18 | 天津和美生物技术有限公司 | 合成多奈哌齐及其衍生物的方法 |
| WO2005076749A2 (en) * | 2004-02-11 | 2005-08-25 | Jubilant Organosys Limited | A novel process for the preparation of 1-benzyl-4-[(5,6-dimethoxy-1-indanon-2-yl)methyl]piperidine |
| US20080114173A1 (en) * | 2004-07-30 | 2008-05-15 | Mathad Vijayavitthal Thippanna | Crystalline Form of Donepezil Hydrochloride |
| AU2005288521A1 (en) | 2004-09-29 | 2006-04-06 | Chemagis Ltd. | Use of purified donepezil maleate for preparing pharmaceutically pure amorphous donepezil hydrochloride |
| US20060122226A1 (en) * | 2004-12-08 | 2006-06-08 | Itai Adin | Crystalline forms of Donepezil base |
| KR100947953B1 (ko) * | 2004-12-30 | 2010-03-15 | 주빌런트 오가노시스 리미티드 | 신규 중간체를 통해1-벤질-4-[(5,6-디메톡시-1-인다논-2-일)메틸]피페리딘또는 이의 염을 제조하는 방법 |
| US8124783B2 (en) * | 2004-12-30 | 2012-02-28 | Jubilant Organosys Limited | Process for producing 1-benzyl-4-[5,6-dimethoxy-1-indanon-2-yl)methyl] piperidine or its salt thereof via novel intermediate |
| WO2006097341A1 (en) * | 2005-03-17 | 2006-09-21 | Synthon B.V. | Process for making crystalline donepezil hydrochloride monohydrate |
| WO2007013922A1 (en) * | 2005-07-20 | 2007-02-01 | Eisai R & D Management Co., Ltd. | 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl] methylpiperidine hydrobromide or crystals thereof |
| EP1906925A1 (de) * | 2005-07-28 | 2008-04-09 | Teikoku Pharma USA, Inc. | Gelierte donezepil-zusammensetzungen und verfahren zu deren herstellung und verwendung |
| CN100436416C (zh) * | 2005-07-29 | 2008-11-26 | 西南合成制药股份有限公司 | 盐酸多奈哌齐合成工艺 |
| GB0515803D0 (en) * | 2005-07-30 | 2005-09-07 | Pliva Hrvatska D O O | Intermediate compounds |
| AR057910A1 (es) | 2005-11-18 | 2007-12-26 | Synthon Bv | Proceso para preparar donepezilo |
| HU227474B1 (en) * | 2005-12-20 | 2011-07-28 | Richter Gedeon Nyrt | Process for industrial scale production of high purity donepezil hydrochloride polymorph i. |
| EP2114166A4 (de) | 2006-12-11 | 2011-05-25 | Reviva Pharmaceuticals Inc | Zusammensetzungen, synthese und verfahren zur verwendung indanonbasierter cholinesterase-hemmer |
| TWI423802B (zh) * | 2007-05-22 | 2014-01-21 | Otsuka Pharma Co Ltd | 用於治療阿茲海默症之藥劑 |
| KR100953038B1 (ko) | 2007-12-12 | 2010-04-14 | 일동제약주식회사 | 염산 도네페질의 개량된 제조방법 |
| AU2009229067B2 (en) | 2008-03-25 | 2013-09-19 | Cipla Limited | Process for the preparation of donepezil hydrochloride |
| US20100105916A1 (en) * | 2008-10-29 | 2010-04-29 | Sterling Biotech Limited | Processes for Preparing Donepezil |
| WO2011151359A1 (en) | 2010-06-02 | 2011-12-08 | Noscira, S.A. | Combined treatment with a cholinesterase inhibitor and a thiadiazolidinedione derivative |
| EP2759536A1 (de) | 2013-01-25 | 2014-07-30 | INSA (Institut National des Sciences Appliquees) de Rouen | Oxidierbare Pyridinderivate, deren Herstellung und Verwendung als Mittel gegen Morbus Alzheimer |
| ES2888074T3 (es) | 2013-08-16 | 2021-12-30 | Univ Maastricht | Tratamiento del deterioro cognitivo con inhibidor de PDE4 |
| US9359315B2 (en) | 2013-09-10 | 2016-06-07 | Arrien Pharmaceuticals Llc | Substituted 2,3-dihydro-1H-inden-1-one retinoic acid-related orphan nuclear receptor antagonists for treating multiple sclerosis |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1542823A (en) * | 1977-01-11 | 1979-03-28 | Ucb Sa | Piperidine derivatives |
| FI95572C (fi) | 1987-06-22 | 1996-02-26 | Eisai Co Ltd | Menetelmä lääkeaineena käyttökelpoisen piperidiinijohdannaisten tai sen farmaseuttisen suolan valmistamiseksi |
| JPH0311063A (ja) * | 1989-06-06 | 1991-01-18 | Denki Kagaku Kogyo Kk | ピペリジン誘導体の製造法 |
| DE4439822A1 (de) * | 1994-11-08 | 1996-08-29 | Bayer Ag | Verfahren zur Herstellung von Benzyl-piperidylmethyl-indanonen |
| AU716462B2 (en) | 1995-12-15 | 2000-02-24 | Pfizer Inc. | Processes and intermediates for preparing 1-benzyl-4-((5,6-dimethoxy-1-indanon)-2-yl)methylpiperidine |
-
1999
- 1999-01-14 WO PCT/JP1999/000111 patent/WO1999036405A1/en not_active Ceased
- 1999-01-14 US US09/582,496 patent/US6252081B1/en not_active Expired - Fee Related
- 1999-01-14 EP EP99900320A patent/EP1047674B1/de not_active Expired - Lifetime
- 1999-01-14 ES ES99900320T patent/ES2237078T3/es not_active Expired - Lifetime
- 1999-01-14 CA CA002316360A patent/CA2316360C/en not_active Expired - Fee Related
- 1999-01-14 AT AT99900320T patent/ATE292116T1/de not_active IP Right Cessation
- 1999-01-14 DE DE69924467T patent/DE69924467T2/de not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| DE69924467T2 (de) | 2006-02-16 |
| US6252081B1 (en) | 2001-06-26 |
| DE69924467D1 (de) | 2005-05-04 |
| CA2316360A1 (en) | 1999-07-22 |
| EP1047674B1 (de) | 2005-03-30 |
| EP1047674A1 (de) | 2000-11-02 |
| CA2316360C (en) | 2007-09-18 |
| ES2237078T3 (es) | 2005-07-16 |
| WO1999036405A1 (en) | 1999-07-22 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| RER | Ceased as to paragraph 5 lit. 3 law introducing patent treaties |