WO2001025201A1 - Procede de preparation de produit intermediaire de paroxetine - Google Patents

Procede de preparation de produit intermediaire de paroxetine Download PDF

Info

Publication number
WO2001025201A1
WO2001025201A1 PCT/GB2000/003797 GB0003797W WO0125201A1 WO 2001025201 A1 WO2001025201 A1 WO 2001025201A1 GB 0003797 W GB0003797 W GB 0003797W WO 0125201 A1 WO0125201 A1 WO 0125201A1
Authority
WO
WIPO (PCT)
Prior art keywords
paroxetine
compound
formula
process according
acid
Prior art date
Application number
PCT/GB2000/003797
Other languages
English (en)
Inventor
David Crowe
Neal Ward
Original Assignee
Smithkline Beecham P.L.C.
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 Smithkline Beecham P.L.C. filed Critical Smithkline Beecham P.L.C.
Priority to AU75424/00A priority Critical patent/AU7542400A/en
Publication of WO2001025201A1 publication Critical patent/WO2001025201A1/fr

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
    • C07D211/68—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 one double bond between ring members or between a ring member and a non-ring member
    • C07D211/70—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 one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms

Definitions

  • Example 2 of WO 98/01424 describes the preparation of compound (1A) by the reaction of l-benzyl-4-(4'-fluorophenyl)- 1,2,3, 6-tetrahydropyridine (2A) with formaldehyde.
  • Compound (2 A) is prepared from l-benzyl-4-(4'-fluorophenyl)-4- hydroxypiperidine (3 A) which is in turn prepared by the reaction of l-benzyl-4- piperidinone (4) and 4-fluorophenylmagnesium bromide.
  • paroxetine especially paroxetine mesylate or paroxetine hydrochloride, obtained using this invention

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

L'invention concerne des composés représentés par la formule (1), dans laquelle R est un groupe benzyle éventuellement substitué. Ces composés sont des produits intermédiaires précieux en vue de l'élaboration de paroxétine, et sont préparés par la mise en réaction d'un composé représenté par la formule (3), dans laquelle R est tel que défini dans la formule (1), et de formaldéhyde dans un milieu acide à température élevée.
PCT/GB2000/003797 1999-10-05 2000-10-04 Procede de preparation de produit intermediaire de paroxetine WO2001025201A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU75424/00A AU7542400A (en) 1999-10-05 2000-10-04 Process for the preparation of paroxetin intermediate

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB9923539.2A GB9923539D0 (en) 1999-10-05 1999-10-05 Novel process
GB9923539.2 1999-10-05

Publications (1)

Publication Number Publication Date
WO2001025201A1 true WO2001025201A1 (fr) 2001-04-12

Family

ID=10862159

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/GB2000/003797 WO2001025201A1 (fr) 1999-10-05 2000-10-04 Procede de preparation de produit intermediaire de paroxetine

Country Status (3)

Country Link
AU (1) AU7542400A (fr)
GB (1) GB9923539D0 (fr)
WO (1) WO2001025201A1 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2001244083B2 (en) * 2000-03-21 2007-02-08 Chr.Hansen A/S Method for supply of starter cultures having a consistent quality

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4007196A (en) * 1973-01-30 1977-02-08 A/S Ferrosan 4-Phenylpiperidine compounds
US5371092A (en) * 1990-11-24 1994-12-06 Beecham Group, P.L.C. Use of paroxetine for the treatment of senile dementia, bulimia, migraine or anorexia
WO1998001424A1 (fr) * 1996-07-08 1998-01-15 Richter Gedeon Vegyészeti Gyár Rt. Derives de n-benzylpiperidine et de tetrahydropyridine

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4007196A (en) * 1973-01-30 1977-02-08 A/S Ferrosan 4-Phenylpiperidine compounds
US5371092A (en) * 1990-11-24 1994-12-06 Beecham Group, P.L.C. Use of paroxetine for the treatment of senile dementia, bulimia, migraine or anorexia
WO1998001424A1 (fr) * 1996-07-08 1998-01-15 Richter Gedeon Vegyészeti Gyár Rt. Derives de n-benzylpiperidine et de tetrahydropyridine

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
ZIERING ET AL.: "Piperidine Derivatives. Part III. 4-Arylpiperidines", J. ORG. CHEM., vol. 12, 1947, pages 894 - 903, XP002158497 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2001244083B2 (en) * 2000-03-21 2007-02-08 Chr.Hansen A/S Method for supply of starter cultures having a consistent quality

Also Published As

Publication number Publication date
GB9923539D0 (en) 1999-12-08
AU7542400A (en) 2001-05-10

Similar Documents

Publication Publication Date Title
EP0994872B9 (fr) Composes 4-phenylpiperidine
JP2002508000A (ja) 胃運動性の３−もしくは４−置換４−（アミノメチル）−ピペリジン誘導体の二環式ベンズアミド
WO2000035873A1 (fr) Procede de preparation de maleate de paroxetine
EP1137646A1 (fr) Derive paroxetinique
CA2164296C (fr) Chimie heterocyclique
AU3433499A (en) Paroxetine maleate
WO2001025201A1 (fr) Procede de preparation de produit intermediaire de paroxetine
US7335380B2 (en) Amlodipine free base
WO2001025202A1 (fr) Procede de preparation d'intermediaire de la paroxetine
CA2330055A1 (fr) Ascorbate de paroxetine
WO2000032595A1 (fr) Processus de production de solvate acetonique d'hydrochlorure de paroxetine
AU3618699A (en) Paroxetine 10-camphorsulfonate for treatment of cns disorders
WO2001012623A1 (fr) Procede de preparation d'hydrochlorure de paroxetine anhydre
WO1999047519A1 (fr) Forme cristalline de la paroxetine
EP1408039A2 (fr) Solvates mixtes de propan-2-ol et de paroxetine
WO2000032596A1 (fr) Sels amines de paroxetine
WO2001017966A1 (fr) Procede de preparation de 1-methyl-3-carbomethoxy-4-(4'-fluorophenyl)-piperidine
MXPA00010435A (en) Paroxetine 10-camphorsulfonate for treatment of cns disorders
WO2001029002A1 (fr) Preparation d'esters de 4-(fluorophenyl)piperidine
WO2001014369A2 (fr) Nouveau procede
WO2001025230A1 (fr) Procede de preparation de solvate acetonique d'hydrochlorure de paroxetine
WO2000078752A1 (fr) Procede de production de chlorhydrate de paroxetine
EP1133492A1 (fr) Procede de fabrication d'hydrochlorure de paroxetine
WO2001025231A1 (fr) Preparation d'un solvate cetonique de chlorhydrate de paroxetine
SI21121A (sl) Prosta baza amlodipina

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A1

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BY BZ CA CH CN CR CU CZ DE DK DM DZ EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NO NZ PL PT RO RU SD SE SG SI SK SL TJ TM TR TT TZ UA UG US UZ VN YU ZA ZW

AL Designated countries for regional patents

Kind code of ref document: A1

Designated state(s): GH GM KE LS MW MZ SD SL SZ TZ UG ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE BF BJ CF CG CI CM GA GN GW ML MR NE SN TD TG

121 Ep: the epo has been informed by wipo that ep was designated in this application
DFPE Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101)
REG Reference to national code

Ref country code: DE

Ref legal event code: 8642

122 Ep: pct application non-entry in european phase
NENP Non-entry into the national phase

Ref country code: JP