VERBESSERTES VERFAHREN ZUR HERSTELLUNG VON 3-(2-(4-(6-FLUOR-1,2-BENZISOXAZOL-3-YL)-1-PIPERIDINYL)ETHYL)-6,7,8,9-TETRAHYDRO-2-METHYL-4H-PYRIDO(1,2-A)PYRIMIDIN-4-ON

VERBESSERTES VERFAHREN ZUR HERSTELLUNG VON 3-(2-(4-(6-FLUOR-1,2-BENZISOXAZOL-3-YL)-1-PIPERIDINYL)ETHYL)-6,7,8,9-TETRAHYDRO-2-METHYL-4H-PYRIDO(1,2-A)PYRIMIDIN-4-ON

The invention relates to a process for the preparation of 3-{2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl}-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one of the Formula (I), and pharmaceutically acceptable acid addition salts thereof by subjecting the oxime of the Formula (...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Hauptverfasser: PONGO, LASZLO, SIMIG, GYULA, KOERTVELYESSY, GYULANE, CLEMENTIS, GYOERGY, SLEGEL, PETER, NAGY, KALMAN, REITER, JOZSEF, KONCZ, LASZLO, BERECZ, GABOR, VERECZKEYNE DONATH, GYOERGYI, SZULAGYI, JANOS
Format: Patent
Sprache:ger
Schlagworte:
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
Online-Zugang:Volltext bestellen
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
container_end_page
container_issue
container_start_page
container_title
container_volume
creator PONGO, LASZLO
SIMIG, GYULA
KOERTVELYESSY, GYULANE
CLEMENTIS, GYOERGY
SLEGEL, PETER
NAGY, KALMAN
REITER, JOZSEF
KONCZ, LASZLO
BERECZ, GABOR
VERECZKEYNE DONATH, GYOERGYI
SZULAGYI, JANOS
description The invention relates to a process for the preparation of 3-{2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl}-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one of the Formula (I), and pharmaceutically acceptable acid addition salts thereof by subjecting the oxime of the Formula (II), to ring-closure in the presence of an alkali hydroxide, alkali carbonate or alkali-C1-4 alkoxide in an inert organic solvent, converting the base of the Formula I thus obtained into an acid addition salt or setting free the base of the Formula I from an acid addition salt thereof which comprises reacting a halogen derivative of the general Formula (XIV), (wherein Hal is halogen) with piperidine oxime derivative of the Formula (V), or an acid addition salt thereof in the presence of a base, and using by the ring-closure of the oxime of the Formula II formed a C1-4-alkanol as inert solvent. The process of the present invention enables the economical preparation of a product having a purity suitable for pharmaceutical purposes.
format Patent
fullrecord <record><control><sourceid>epo_EVB</sourceid><recordid>TN_cdi_epo_espacenet_DE60219957TT8</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>DE60219957TT8</sourcerecordid><originalsourceid>FETCH-epo_espacenet_DE60219957TT83</originalsourceid><addsrcrecordid>eNqNjMtqwkAYhbPpQqzvMHQVIQeaS6NZxuZPJzDOhH8mYrIRKdOVWME-kU_aRHwAV4fv3GbBbUe8IWuJHVkxQl1KJi2GjoUkto6U6vSX2BktUoQJwgxhjlp1hhFHCTakh8aafTkYhRS9WiJG27TETdXoEcnJycyjVbSOCjhyXMq-YoME23uITKLtx74Jp8dyOcF2miOD0a_By8_xdPWLh86Dt5rcp4S__B789XL89mf_d6gof0_iovhYObdOnyr9A5gHRJ0</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>patent</recordtype></control><display><type>patent</type><title>VERBESSERTES VERFAHREN ZUR HERSTELLUNG VON 3-(2-(4-(6-FLUOR-1,2-BENZISOXAZOL-3-YL)-1-PIPERIDINYL)ETHYL)-6,7,8,9-TETRAHYDRO-2-METHYL-4H-PYRIDO(1,2-A)PYRIMIDIN-4-ON</title><source>esp@cenet</source><creator>PONGO, LASZLO ; SIMIG, GYULA ; KOERTVELYESSY, GYULANE ; CLEMENTIS, GYOERGY ; SLEGEL, PETER ; NAGY, KALMAN ; REITER, JOZSEF ; KONCZ, LASZLO ; BERECZ, GABOR ; VERECZKEYNE DONATH, GYOERGYI ; SZULAGYI, JANOS</creator><creatorcontrib>PONGO, LASZLO ; SIMIG, GYULA ; KOERTVELYESSY, GYULANE ; CLEMENTIS, GYOERGY ; SLEGEL, PETER ; NAGY, KALMAN ; REITER, JOZSEF ; KONCZ, LASZLO ; BERECZ, GABOR ; VERECZKEYNE DONATH, GYOERGYI ; SZULAGYI, JANOS</creatorcontrib><description>The invention relates to a process for the preparation of 3-{2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl}-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one of the Formula (I), and pharmaceutically acceptable acid addition salts thereof by subjecting the oxime of the Formula (II), to ring-closure in the presence of an alkali hydroxide, alkali carbonate or alkali-C1-4 alkoxide in an inert organic solvent, converting the base of the Formula I thus obtained into an acid addition salt or setting free the base of the Formula I from an acid addition salt thereof which comprises reacting a halogen derivative of the general Formula (XIV), (wherein Hal is halogen) with piperidine oxime derivative of the Formula (V), or an acid addition salt thereof in the presence of a base, and using by the ring-closure of the oxime of the Formula II formed a C1-4-alkanol as inert solvent. The process of the present invention enables the economical preparation of a product having a purity suitable for pharmaceutical purposes.</description><language>ger</language><subject>CHEMISTRY ; HETEROCYCLIC COMPOUNDS ; METALLURGY ; ORGANIC CHEMISTRY</subject><creationdate>2008</creationdate><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&amp;date=20080424&amp;DB=EPODOC&amp;CC=DE&amp;NR=60219957T8$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,776,881,25543,76294</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&amp;date=20080424&amp;DB=EPODOC&amp;CC=DE&amp;NR=60219957T8$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>PONGO, LASZLO</creatorcontrib><creatorcontrib>SIMIG, GYULA</creatorcontrib><creatorcontrib>KOERTVELYESSY, GYULANE</creatorcontrib><creatorcontrib>CLEMENTIS, GYOERGY</creatorcontrib><creatorcontrib>SLEGEL, PETER</creatorcontrib><creatorcontrib>NAGY, KALMAN</creatorcontrib><creatorcontrib>REITER, JOZSEF</creatorcontrib><creatorcontrib>KONCZ, LASZLO</creatorcontrib><creatorcontrib>BERECZ, GABOR</creatorcontrib><creatorcontrib>VERECZKEYNE DONATH, GYOERGYI</creatorcontrib><creatorcontrib>SZULAGYI, JANOS</creatorcontrib><title>VERBESSERTES VERFAHREN ZUR HERSTELLUNG VON 3-(2-(4-(6-FLUOR-1,2-BENZISOXAZOL-3-YL)-1-PIPERIDINYL)ETHYL)-6,7,8,9-TETRAHYDRO-2-METHYL-4H-PYRIDO(1,2-A)PYRIMIDIN-4-ON</title><description>The invention relates to a process for the preparation of 3-{2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl}-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one of the Formula (I), and pharmaceutically acceptable acid addition salts thereof by subjecting the oxime of the Formula (II), to ring-closure in the presence of an alkali hydroxide, alkali carbonate or alkali-C1-4 alkoxide in an inert organic solvent, converting the base of the Formula I thus obtained into an acid addition salt or setting free the base of the Formula I from an acid addition salt thereof which comprises reacting a halogen derivative of the general Formula (XIV), (wherein Hal is halogen) with piperidine oxime derivative of the Formula (V), or an acid addition salt thereof in the presence of a base, and using by the ring-closure of the oxime of the Formula II formed a C1-4-alkanol as inert solvent. The process of the present invention enables the economical preparation of a product having a purity suitable for pharmaceutical purposes.</description><subject>CHEMISTRY</subject><subject>HETEROCYCLIC COMPOUNDS</subject><subject>METALLURGY</subject><subject>ORGANIC CHEMISTRY</subject><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>2008</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNqNjMtqwkAYhbPpQqzvMHQVIQeaS6NZxuZPJzDOhH8mYrIRKdOVWME-kU_aRHwAV4fv3GbBbUe8IWuJHVkxQl1KJi2GjoUkto6U6vSX2BktUoQJwgxhjlp1hhFHCTakh8aafTkYhRS9WiJG27TETdXoEcnJycyjVbSOCjhyXMq-YoME23uITKLtx74Jp8dyOcF2miOD0a_By8_xdPWLh86Dt5rcp4S__B789XL89mf_d6gof0_iovhYObdOnyr9A5gHRJ0</recordid><startdate>20080424</startdate><enddate>20080424</enddate><creator>PONGO, LASZLO</creator><creator>SIMIG, GYULA</creator><creator>KOERTVELYESSY, GYULANE</creator><creator>CLEMENTIS, GYOERGY</creator><creator>SLEGEL, PETER</creator><creator>NAGY, KALMAN</creator><creator>REITER, JOZSEF</creator><creator>KONCZ, LASZLO</creator><creator>BERECZ, GABOR</creator><creator>VERECZKEYNE DONATH, GYOERGYI</creator><creator>SZULAGYI, JANOS</creator><scope>EVB</scope></search><sort><creationdate>20080424</creationdate><title>VERBESSERTES VERFAHREN ZUR HERSTELLUNG VON 3-(2-(4-(6-FLUOR-1,2-BENZISOXAZOL-3-YL)-1-PIPERIDINYL)ETHYL)-6,7,8,9-TETRAHYDRO-2-METHYL-4H-PYRIDO(1,2-A)PYRIMIDIN-4-ON</title><author>PONGO, LASZLO ; SIMIG, GYULA ; KOERTVELYESSY, GYULANE ; CLEMENTIS, GYOERGY ; SLEGEL, PETER ; NAGY, KALMAN ; REITER, JOZSEF ; KONCZ, LASZLO ; BERECZ, GABOR ; VERECZKEYNE DONATH, GYOERGYI ; SZULAGYI, JANOS</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_DE60219957TT83</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>ger</language><creationdate>2008</creationdate><topic>CHEMISTRY</topic><topic>HETEROCYCLIC COMPOUNDS</topic><topic>METALLURGY</topic><topic>ORGANIC CHEMISTRY</topic><toplevel>online_resources</toplevel><creatorcontrib>PONGO, LASZLO</creatorcontrib><creatorcontrib>SIMIG, GYULA</creatorcontrib><creatorcontrib>KOERTVELYESSY, GYULANE</creatorcontrib><creatorcontrib>CLEMENTIS, GYOERGY</creatorcontrib><creatorcontrib>SLEGEL, PETER</creatorcontrib><creatorcontrib>NAGY, KALMAN</creatorcontrib><creatorcontrib>REITER, JOZSEF</creatorcontrib><creatorcontrib>KONCZ, LASZLO</creatorcontrib><creatorcontrib>BERECZ, GABOR</creatorcontrib><creatorcontrib>VERECZKEYNE DONATH, GYOERGYI</creatorcontrib><creatorcontrib>SZULAGYI, JANOS</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>PONGO, LASZLO</au><au>SIMIG, GYULA</au><au>KOERTVELYESSY, GYULANE</au><au>CLEMENTIS, GYOERGY</au><au>SLEGEL, PETER</au><au>NAGY, KALMAN</au><au>REITER, JOZSEF</au><au>KONCZ, LASZLO</au><au>BERECZ, GABOR</au><au>VERECZKEYNE DONATH, GYOERGYI</au><au>SZULAGYI, JANOS</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>VERBESSERTES VERFAHREN ZUR HERSTELLUNG VON 3-(2-(4-(6-FLUOR-1,2-BENZISOXAZOL-3-YL)-1-PIPERIDINYL)ETHYL)-6,7,8,9-TETRAHYDRO-2-METHYL-4H-PYRIDO(1,2-A)PYRIMIDIN-4-ON</title><date>2008-04-24</date><risdate>2008</risdate><abstract>The invention relates to a process for the preparation of 3-{2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl}-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one of the Formula (I), and pharmaceutically acceptable acid addition salts thereof by subjecting the oxime of the Formula (II), to ring-closure in the presence of an alkali hydroxide, alkali carbonate or alkali-C1-4 alkoxide in an inert organic solvent, converting the base of the Formula I thus obtained into an acid addition salt or setting free the base of the Formula I from an acid addition salt thereof which comprises reacting a halogen derivative of the general Formula (XIV), (wherein Hal is halogen) with piperidine oxime derivative of the Formula (V), or an acid addition salt thereof in the presence of a base, and using by the ring-closure of the oxime of the Formula II formed a C1-4-alkanol as inert solvent. The process of the present invention enables the economical preparation of a product having a purity suitable for pharmaceutical purposes.</abstract><oa>free_for_read</oa></addata></record>
fulltext fulltext_linktorsrc
identifier
ispartof
issn
language ger
recordid cdi_epo_espacenet_DE60219957TT8
source esp@cenet
subjects CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
title VERBESSERTES VERFAHREN ZUR HERSTELLUNG VON 3-(2-(4-(6-FLUOR-1,2-BENZISOXAZOL-3-YL)-1-PIPERIDINYL)ETHYL)-6,7,8,9-TETRAHYDRO-2-METHYL-4H-PYRIDO(1,2-A)PYRIMIDIN-4-ON
url https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-01-22T07%3A44%3A16IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-epo_EVB&rft_val_fmt=info:ofi/fmt:kev:mtx:patent&rft.genre=patent&rft.au=PONGO,%20LASZLO&rft.date=2008-04-24&rft_id=info:doi/&rft_dat=%3Cepo_EVB%3EDE60219957TT8%3C/epo_EVB%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_id=info:pmid/&rfr_iscdi=true