AR063319A1 - IMPROVED PROCESS TO PREPARE THE POLYMORPHIC FORM I OF DONEPEZYL CHLORHYDRATE (2,3-DIHYDRO-5,6-DIMETOXI-2 - [[1- (PHENYLMETHYL) -4-PIPERIDIN] METHYL-1H-INDEN-1-ONA) - Google Patents

IMPROVED PROCESS TO PREPARE THE POLYMORPHIC FORM I OF DONEPEZYL CHLORHYDRATE (2,3-DIHYDRO-5,6-DIMETOXI-2 - [[1- (PHENYLMETHYL) -4-PIPERIDIN] METHYL-1H-INDEN-1-ONA)

Info

Publication number
AR063319A1
AR063319A1 ARP070104582A ARP070104582A AR063319A1 AR 063319 A1 AR063319 A1 AR 063319A1 AR P070104582 A ARP070104582 A AR P070104582A AR P070104582 A ARP070104582 A AR P070104582A AR 063319 A1 AR063319 A1 AR 063319A1
Authority
AR
Argentina
Prior art keywords
polymorphic form
donepezyl
dimetoxi
chlorhydrate
inden
Prior art date
Application number
ARP070104582A
Other languages
Spanish (es)
Inventor
Madrid Nuria Soldevilla
Original Assignee
Medichem Sa
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
Application filed by Medichem Sa filed Critical Medichem Sa
Publication of AR063319A1 publication Critical patent/AR063319A1/en

Links

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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

Abstract

Reivindicacion 1: Un proceso para preparar una forma polimorfica 1 de clorhidrato de donepezilo que es muy estable respecto de la conversion en otras formas polimorficas, caracterizado porque comprende: i. disolver clorhidrato de donepezilo en metanol y una pequena cantidad de agua con calentamiento; ii. enfriar la solucion; iii. poner en contacto la solucion del paso (ji) con al menos un solvente no polar, o mezclas de dichos solventes; iv. aislar la forma polimorfica 1 humeda de clorhidrato de donepezilo obtenida en el paso (iii); y v. eliminar al menos una porcion del metanol residual de la forma poIimorfica 1 humeda de clorhidrato de donepezilo obtenida en el paso (iv).Claim 1: A process for preparing a polymorphic form 1 of donepezil hydrochloride that is very stable with respect to conversion into other polymorphic forms, characterized in that it comprises: i. dissolve donepezil hydrochloride in methanol and a small amount of water with heating; ii. cool the solution; iii. contacting the solution of step (ji) with at least one non-polar solvent, or mixtures of said solvents; iv. isolate the wet polymorphic form 1 of donepezil hydrochloride obtained in step (iii); and V. remove at least a portion of the residual methanol in the wet polymorphic form 1 of donepezil hydrochloride obtained in step (iv).

ARP070104582A 2006-10-16 2007-10-16 IMPROVED PROCESS TO PREPARE THE POLYMORPHIC FORM I OF DONEPEZYL CHLORHYDRATE (2,3-DIHYDRO-5,6-DIMETOXI-2 - [[1- (PHENYLMETHYL) -4-PIPERIDIN] METHYL-1H-INDEN-1-ONA) AR063319A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US85175706P 2006-10-16 2006-10-16
US92919507P 2007-06-18 2007-06-18

Publications (1)

Publication Number Publication Date
AR063319A1 true AR063319A1 (en) 2009-01-21

Family

ID=39712458

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP070104582A AR063319A1 (en) 2006-10-16 2007-10-16 IMPROVED PROCESS TO PREPARE THE POLYMORPHIC FORM I OF DONEPEZYL CHLORHYDRATE (2,3-DIHYDRO-5,6-DIMETOXI-2 - [[1- (PHENYLMETHYL) -4-PIPERIDIN] METHYL-1H-INDEN-1-ONA)

Country Status (2)

Country Link
AR (1) AR063319A1 (en)
WO (1) WO2008117123A2 (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102060752B (en) * 2011-01-24 2013-03-13 上海右手医药科技开发有限公司 Method for producing high-purity donepezil hydrochloride anhydrous I type crystal form and product thereof
CN103694164B (en) * 2014-01-23 2015-08-12 天津大学 A kind of New crystal form of donepezil hydrochloride and preparation method

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU1153097A (en) * 1996-06-07 1998-01-05 Eisai Co. Ltd. Stable polymorphs of donepezil (1-benzyl-4-{(5,6-dimethoxy-1-indanon)-2-yl}methylpiperidine ) hydrochloride and process for production
EP1858847A1 (en) * 2005-02-28 2007-11-28 Ranbaxy Laboratories Limited Stable form i donepezil hydrochloride and process for its preparation and use in pharmaceutical compositions
CN101410374A (en) * 2005-11-14 2009-04-15 麦迪凯姆股份公司 Synthesis and preparations of intermediates and polymorphs thereof useful for the preparation of donepezil hydrochloride
HU227474B1 (en) * 2005-12-20 2011-07-28 Richter Gedeon Nyrt Process for industrial scale production of high purity donepezil hydrochloride polymorph i.

Also Published As

Publication number Publication date
WO2008117123A2 (en) 2008-10-02
WO2008117123A3 (en) 2008-12-04

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