HUP9904275A2 - Eljárás 1-benzil-4-[(5,6-dimetoxi-1-indanon)-2-il]-metil-piperidin-származékok előállítására,valamint az előállításnál használt köztitermékek - Google Patents
Eljárás 1-benzil-4-[(5,6-dimetoxi-1-indanon)-2-il]-metil-piperidin-származékok előállítására,valamint az előállításnál használt köztitermékekInfo
- Publication number
- HUP9904275A2 HUP9904275A2 HU9904275A HUP9904275A HUP9904275A2 HU P9904275 A2 HUP9904275 A2 HU P9904275A2 HU 9904275 A HU9904275 A HU 9904275A HU P9904275 A HUP9904275 A HU P9904275A HU P9904275 A2 HUP9904275 A2 HU P9904275A2
- Authority
- HU
- Hungary
- Prior art keywords
- formula
- compound
- carbon atoms
- general formula
- pipe
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 4
- 239000000543 intermediate Substances 0.000 title abstract 2
- PAMIQIKDUOTOBW-UHFFFAOYSA-N 1-methylpiperidine Chemical compound CN1CCCCC1 PAMIQIKDUOTOBW-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 8
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 125000004432 carbon atom Chemical group C* 0.000 abstract 4
- 239000000428 dust Substances 0.000 abstract 3
- 239000000843 powder Substances 0.000 abstract 2
- 102000012440 Acetylcholinesterase Human genes 0.000 abstract 1
- 108010022752 Acetylcholinesterase Proteins 0.000 abstract 1
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 229940022698 acetylcholinesterase Drugs 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- -1 benzyl halide Chemical class 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-M hydroxide Chemical compound [OH-] XLYOFNOQVPJJNP-UHFFFAOYSA-M 0.000 abstract 1
- 239000013067 intermediate product Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- 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)
- Hydrogenated Pyridines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
A találmány a (Vll) képletű 1-benzil-[5,6-demetőxi-1-indanőn)-2- il]-metil-piperidin előállítására vőnatkőzó eljárásőkra, valamint azeljárásőknál hasznősítőtt köztitermékekre vőnatkőzik. A találmánytöbbek között eljárást biztősít az (I) általánős képletű vegyületek -a képletben R1 jelentése R1O(C=O)- vagy R3(C=O)- képletű csőpőrt, R2jelentése 1-4 szénatőmőt tartalmazó alkilcsőpőrt és R3 jelentése 1-4szénatőmőt tartalmazó alkilcsőpőrt vagy őlyan fenilcsőpőrt, amelyadőtt esetben szűbsztitűálva van 1-3 szűbsztitűenssel, éspedigegymástól függetlenül megválasztva 1-4 szénatőmőt tartalmazó alkil-,1-4 szénatőmőt tartalmazó alkőxi- és tritlűőr-metilcsőpőrtők éshalőgénatőmők közül megválasztőtt szűbsztitűensekkel - előállítására,mely abban áll, hőgy egy (III) általánős képletű vegyületet - aképletben R1 jelentése a fenti - egy metenilezőszerrel reagáltatnak,majd egy így kapőtt (II) általánős képletű vegyületet - a képletben R1jelentése a kőrábban megadőtt egy erős savval kezelnek. Ezűtán egy ígykapőtt (I) általánős képletű vegyületet egy hidrőxiddal kezelve a (VI)képletű vegyület, majd az űtóbbit egy benzil-halőgeniddel egy bázisjelenlétében reagáltatva a (VII) képletű célvegyület állítható elő. Atalálmány az új (I), (II) és (III) általánős képletű köztitermékekreis vőnatkőzik. A (VII) képletű vegyület és gyógyászatilag elfőgadhatósói felhasználhatók acetilkőlin-észteráz-aktivitás által őkőzőttbetegségek, példáűl az Alzheimer-kór kezelésére. ŕ
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US875395P | 1995-12-15 | 1995-12-15 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HUP9904275A2 true HUP9904275A2 (hu) | 2000-05-28 |
| HUP9904275A3 HUP9904275A3 (en) | 2001-05-28 |
Family
ID=21733469
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU9904275A HUP9904275A3 (en) | 1995-12-15 | 1996-10-11 | Processes and intermediates for preparing 1-benzyl-4-(5,6-dimethoxy-1-indanon)-2-yl)methylpiperidine |
Country Status (33)
| Country | Link |
|---|---|
| EP (1) | EP0883607A1 (hu) |
| JP (1) | JP3066083B2 (hu) |
| KR (1) | KR20000064387A (hu) |
| AP (1) | AP708A (hu) |
| AR (1) | AR004368A1 (hu) |
| AU (1) | AU716462B2 (hu) |
| BG (1) | BG102525A (hu) |
| BR (1) | BR9612018A (hu) |
| CA (1) | CA2237647A1 (hu) |
| CO (1) | CO4750831A1 (hu) |
| CZ (1) | CZ180898A3 (hu) |
| DZ (1) | DZ2141A1 (hu) |
| GT (1) | GT199600092A (hu) |
| HN (1) | HN1996000065A (hu) |
| HR (1) | HRP960592A2 (hu) |
| HU (1) | HUP9904275A3 (hu) |
| IL (3) | IL136421A0 (hu) |
| IS (1) | IS4752A (hu) |
| MA (1) | MA24032A1 (hu) |
| NO (1) | NO982712L (hu) |
| NZ (1) | NZ318843A (hu) |
| OA (1) | OA10694A (hu) |
| PE (1) | PE25698A1 (hu) |
| PL (1) | PL197306B1 (hu) |
| RO (1) | RO121382B1 (hu) |
| RU (1) | RU2160731C2 (hu) |
| SK (1) | SK75498A3 (hu) |
| TN (1) | TNSN96153A1 (hu) |
| TW (1) | TW414787B (hu) |
| UY (1) | UY24401A1 (hu) |
| WO (1) | WO1997022584A1 (hu) |
| YU (1) | YU49486B (hu) |
| ZA (1) | ZA9610533B (hu) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1999036405A1 (en) | 1998-01-16 | 1999-07-22 | Eisai Co., Ltd. | Process for production of donepezil derivative |
| IL125809A (en) * | 1998-08-17 | 2005-08-31 | Finetech Lab Ltd | Process and intermediates for production of donepezil and related compounds |
| US7148354B2 (en) * | 2002-07-24 | 2006-12-12 | Dr. Reddy's Laboratories Limited | Process for preparation of donepezil |
| IL150982A (en) | 2002-07-30 | 2007-02-11 | Ori Lerman | Process for making Donafzil |
| IL151253A0 (en) * | 2002-08-14 | 2003-04-10 | Finetech Lab Ltd | Process for production of highly pure donepezil hydrochloride |
| 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 (en) * | 2003-03-21 | 2005-12-28 | Ranbaxy Laboratories, Ltd. | Process for the preparation of donepezil and derivatives thereof |
| WO2004099142A1 (en) * | 2003-05-05 | 2004-11-18 | Ranbaxy Laboratories Limited | Hydrobromide salt of benzyl-piperidylmethyl-indanone and its polymorphs |
| AU2003247158A1 (en) | 2003-07-01 | 2005-01-21 | Hetero Drugs Limited | Preparation of intermediates for acetyl cholinesterase inhibitors |
| 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 |
| JP2008514691A (ja) | 2004-09-29 | 2008-05-08 | ケマジス リミティド | 薬学的に純粋な非晶質塩酸ドネペジルを製造するための精製されたマレイン酸ドネペジルの使用 |
| 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 |
| ES2354737T3 (es) | 2006-01-04 | 2011-03-17 | Cipla Limited | Procedimiento y producto intermedio para la preparación de donepezylo. |
| BRPI0720211A2 (pt) * | 2006-12-11 | 2013-12-24 | Reviva Pharmaceuticals Inc | Derivado de indanona, composição, e, uso de uma composição |
| WO2013078608A1 (en) * | 2011-11-29 | 2013-06-06 | Ziqiang Gu | Donepezil pamoate and methods of making and using the same |
| AU2014307803A1 (en) | 2013-08-16 | 2016-03-10 | Universiteit Maastricht | Treatment of cognitive impairment with PDE4 inhibitor |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FI95572C (fi) * | 1987-06-22 | 1996-02-26 | Eisai Co Ltd | Menetelmä lääkeaineena käyttökelpoisen piperidiinijohdannaisten tai sen farmaseuttisen suolan valmistamiseksi |
| FR2642069B1 (fr) * | 1989-01-20 | 1991-04-12 | Rhone Poulenc Sante | Nouveaux derives du benzopyranne, leur preparation et les compositions pharmaceutiques qui les contiennent |
| DE4439822A1 (de) * | 1994-11-08 | 1996-08-29 | Bayer Ag | Verfahren zur Herstellung von Benzyl-piperidylmethyl-indanonen |
-
1996
- 1996-10-11 SK SK754-98A patent/SK75498A3/sk unknown
- 1996-10-11 IL IL13642196A patent/IL136421A0/xx unknown
- 1996-10-11 CA CA002237647A patent/CA2237647A1/en not_active Abandoned
- 1996-10-11 KR KR1019980704423A patent/KR20000064387A/ko not_active Application Discontinuation
- 1996-10-11 BR BR9612018A patent/BR9612018A/pt not_active Application Discontinuation
- 1996-10-11 IL IL12445296A patent/IL124452A0/xx unknown
- 1996-10-11 WO PCT/IB1996/001076 patent/WO1997022584A1/en not_active Application Discontinuation
- 1996-10-11 IL IL13642096A patent/IL136420A0/xx unknown
- 1996-10-11 RO RO98-01070A patent/RO121382B1/ro unknown
- 1996-10-11 PL PL327512A patent/PL197306B1/pl not_active IP Right Cessation
- 1996-10-11 RU RU98111204/04A patent/RU2160731C2/ru not_active IP Right Cessation
- 1996-10-11 CZ CZ981808A patent/CZ180898A3/cs unknown
- 1996-10-11 JP JP9522607A patent/JP3066083B2/ja not_active Expired - Lifetime
- 1996-10-11 NZ NZ318843A patent/NZ318843A/xx unknown
- 1996-10-11 EP EP96931937A patent/EP0883607A1/en not_active Withdrawn
- 1996-10-11 AU AU70925/96A patent/AU716462B2/en not_active Ceased
- 1996-10-11 HU HU9904275A patent/HUP9904275A3/hu unknown
- 1996-10-14 TW TW085112515A patent/TW414787B/zh not_active IP Right Cessation
- 1996-10-15 HN HN1996000065A patent/HN1996000065A/es unknown
- 1996-11-18 GT GT199600092A patent/GT199600092A/es unknown
- 1996-12-09 PE PE1996000883A patent/PE25698A1/es not_active Application Discontinuation
- 1996-12-10 AR ARP960105577A patent/AR004368A1/es unknown
- 1996-12-11 YU YU66096A patent/YU49486B/sh unknown
- 1996-12-11 DZ DZ960186A patent/DZ2141A1/fr active
- 1996-12-11 MA MA24424A patent/MA24032A1/fr unknown
- 1996-12-11 TN TNTNSN96153A patent/TNSN96153A1/fr unknown
- 1996-12-12 AP APAP/P/1996/000892A patent/AP708A/en active
- 1996-12-12 UY UY24401A patent/UY24401A1/es not_active IP Right Cessation
- 1996-12-12 CO CO96065334A patent/CO4750831A1/es unknown
- 1996-12-13 ZA ZA9610533A patent/ZA9610533B/xx unknown
- 1996-12-13 HR HR60/008,753A patent/HRP960592A2/xx not_active Application Discontinuation
-
1998
- 1998-05-22 IS IS4752A patent/IS4752A/is unknown
- 1998-06-05 OA OA9800076A patent/OA10694A/en unknown
- 1998-06-09 BG BG102525A patent/BG102525A/xx unknown
- 1998-06-12 NO NO982712A patent/NO982712L/no not_active Application Discontinuation
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FD9A | Lapse of provisional protection due to non-payment of fees |