EXEMESTANE AND ITS INTERMEDIATES AND METHODS OF MAKING THE SAME

EXEMESTANE AND ITS INTERMEDIATES AND METHODS OF MAKING THE SAME

A method is provided for preparing an aromatase inhibitor of formula (I) wherein each of R1, R2, R3, R4, independently, is hydrogen, halogen or C1-C6 alkyl. In one form, the aromatase inhibitor is exemestane wherein each of R1, R2, R3, R4 is hydrogen. In the method, a compound of formula (II) wherei...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Hauptverfasser: PASCONE, JOHN, M, STEHLE, NATHAN, W, PARIZA, RICHARD, J, WEIS, SCOT, W, ZIZELMAN, PAUL, VAN ORNUM, SCOTT, G, KUNNEN, KEVIN
Format: Patent
Sprache:eng ; fre ; ger
Schlagworte:
CHEMISTRY
METALLURGY
ORGANIC CHEMISTRY
STEROIDS
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 PASCONE, JOHN, M
STEHLE, NATHAN, W
PARIZA, RICHARD, J
WEIS, SCOT, W
ZIZELMAN, PAUL
VAN ORNUM, SCOTT, G
KUNNEN, KEVIN
description A method is provided for preparing an aromatase inhibitor of formula (I) wherein each of R1, R2, R3, R4, independently, is hydrogen, halogen or C1-C6 alkyl. In one form, the aromatase inhibitor is exemestane wherein each of R1, R2, R3, R4 is hydrogen. In the method, a compound of formula (II) wherein R1, R2, R3, R4 are as defined above and R is alkylene, is reacted with a deprotonating agent and a compound of the formula R5SO2X wherein R5 is C1-C5 alkyl and X is halogen so as to obtain a compound of formula (III) wherein R1, R2, R3, R4, R5 are as defined above. The compound of Formula (III) is then reacted with a base to form an aromatase inhibitor of formula (I).
format Patent
fullrecord <record><control><sourceid>epo_EVB</sourceid><recordid>TN_cdi_epo_espacenet_EP1709062A1</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>EP1709062A1</sourcerecordid><originalsourceid>FETCH-epo_espacenet_EP1709062A13</originalsourceid><addsrcrecordid>eNrjZLB3jXD1dQ0OcfRzVXD0c1HwDAlW8PQLcQ3ydXXxdAxxDQaL-rqGePi7BCv4uyn4Onp7-rkrhHi4KgQ7-rryMLCmJeYUp_JCaW4GBTfXEGcP3dSC_PjU4oLE5NS81JJ41wBDcwNLAzMjR0NjIpQAAAw9KZo</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>patent</recordtype></control><display><type>patent</type><title>EXEMESTANE AND ITS INTERMEDIATES AND METHODS OF MAKING THE SAME</title><source>esp@cenet</source><creator>PASCONE, JOHN, M ; STEHLE, NATHAN, W ; PARIZA, RICHARD, J ; WEIS, SCOT, W ; ZIZELMAN, PAUL ; VAN ORNUM, SCOTT, G ; KUNNEN, KEVIN</creator><creatorcontrib>PASCONE, JOHN, M ; STEHLE, NATHAN, W ; PARIZA, RICHARD, J ; WEIS, SCOT, W ; ZIZELMAN, PAUL ; VAN ORNUM, SCOTT, G ; KUNNEN, KEVIN</creatorcontrib><description>A method is provided for preparing an aromatase inhibitor of formula (I) wherein each of R1, R2, R3, R4, independently, is hydrogen, halogen or C1-C6 alkyl. In one form, the aromatase inhibitor is exemestane wherein each of R1, R2, R3, R4 is hydrogen. In the method, a compound of formula (II) wherein R1, R2, R3, R4 are as defined above and R is alkylene, is reacted with a deprotonating agent and a compound of the formula R5SO2X wherein R5 is C1-C5 alkyl and X is halogen so as to obtain a compound of formula (III) wherein R1, R2, R3, R4, R5 are as defined above. The compound of Formula (III) is then reacted with a base to form an aromatase inhibitor of formula (I).</description><language>eng ; fre ; ger</language><subject>CHEMISTRY ; METALLURGY ; ORGANIC CHEMISTRY ; STEROIDS</subject><creationdate>2006</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=20061011&amp;DB=EPODOC&amp;CC=EP&amp;NR=1709062A1$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,780,885,25564,76547</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&amp;date=20061011&amp;DB=EPODOC&amp;CC=EP&amp;NR=1709062A1$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>PASCONE, JOHN, M</creatorcontrib><creatorcontrib>STEHLE, NATHAN, W</creatorcontrib><creatorcontrib>PARIZA, RICHARD, J</creatorcontrib><creatorcontrib>WEIS, SCOT, W</creatorcontrib><creatorcontrib>ZIZELMAN, PAUL</creatorcontrib><creatorcontrib>VAN ORNUM, SCOTT, G</creatorcontrib><creatorcontrib>KUNNEN, KEVIN</creatorcontrib><title>EXEMESTANE AND ITS INTERMEDIATES AND METHODS OF MAKING THE SAME</title><description>A method is provided for preparing an aromatase inhibitor of formula (I) wherein each of R1, R2, R3, R4, independently, is hydrogen, halogen or C1-C6 alkyl. In one form, the aromatase inhibitor is exemestane wherein each of R1, R2, R3, R4 is hydrogen. In the method, a compound of formula (II) wherein R1, R2, R3, R4 are as defined above and R is alkylene, is reacted with a deprotonating agent and a compound of the formula R5SO2X wherein R5 is C1-C5 alkyl and X is halogen so as to obtain a compound of formula (III) wherein R1, R2, R3, R4, R5 are as defined above. The compound of Formula (III) is then reacted with a base to form an aromatase inhibitor of formula (I).</description><subject>CHEMISTRY</subject><subject>METALLURGY</subject><subject>ORGANIC CHEMISTRY</subject><subject>STEROIDS</subject><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>2006</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNrjZLB3jXD1dQ0OcfRzVXD0c1HwDAlW8PQLcQ3ydXXxdAxxDQaL-rqGePi7BCv4uyn4Onp7-rkrhHi4KgQ7-rryMLCmJeYUp_JCaW4GBTfXEGcP3dSC_PjU4oLE5NS81JJ41wBDcwNLAzMjR0NjIpQAAAw9KZo</recordid><startdate>20061011</startdate><enddate>20061011</enddate><creator>PASCONE, JOHN, M</creator><creator>STEHLE, NATHAN, W</creator><creator>PARIZA, RICHARD, J</creator><creator>WEIS, SCOT, W</creator><creator>ZIZELMAN, PAUL</creator><creator>VAN ORNUM, SCOTT, G</creator><creator>KUNNEN, KEVIN</creator><scope>EVB</scope></search><sort><creationdate>20061011</creationdate><title>EXEMESTANE AND ITS INTERMEDIATES AND METHODS OF MAKING THE SAME</title><author>PASCONE, JOHN, M ; STEHLE, NATHAN, W ; PARIZA, RICHARD, J ; WEIS, SCOT, W ; ZIZELMAN, PAUL ; VAN ORNUM, SCOTT, G ; KUNNEN, KEVIN</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_EP1709062A13</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng ; fre ; ger</language><creationdate>2006</creationdate><topic>CHEMISTRY</topic><topic>METALLURGY</topic><topic>ORGANIC CHEMISTRY</topic><topic>STEROIDS</topic><toplevel>online_resources</toplevel><creatorcontrib>PASCONE, JOHN, M</creatorcontrib><creatorcontrib>STEHLE, NATHAN, W</creatorcontrib><creatorcontrib>PARIZA, RICHARD, J</creatorcontrib><creatorcontrib>WEIS, SCOT, W</creatorcontrib><creatorcontrib>ZIZELMAN, PAUL</creatorcontrib><creatorcontrib>VAN ORNUM, SCOTT, G</creatorcontrib><creatorcontrib>KUNNEN, KEVIN</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>PASCONE, JOHN, M</au><au>STEHLE, NATHAN, W</au><au>PARIZA, RICHARD, J</au><au>WEIS, SCOT, W</au><au>ZIZELMAN, PAUL</au><au>VAN ORNUM, SCOTT, G</au><au>KUNNEN, KEVIN</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>EXEMESTANE AND ITS INTERMEDIATES AND METHODS OF MAKING THE SAME</title><date>2006-10-11</date><risdate>2006</risdate><abstract>A method is provided for preparing an aromatase inhibitor of formula (I) wherein each of R1, R2, R3, R4, independently, is hydrogen, halogen or C1-C6 alkyl. In one form, the aromatase inhibitor is exemestane wherein each of R1, R2, R3, R4 is hydrogen. In the method, a compound of formula (II) wherein R1, R2, R3, R4 are as defined above and R is alkylene, is reacted with a deprotonating agent and a compound of the formula R5SO2X wherein R5 is C1-C5 alkyl and X is halogen so as to obtain a compound of formula (III) wherein R1, R2, R3, R4, R5 are as defined above. The compound of Formula (III) is then reacted with a base to form an aromatase inhibitor of formula (I).</abstract><oa>free_for_read</oa></addata></record>
fulltext fulltext_linktorsrc
identifier
ispartof
issn
language eng ; fre ; ger
recordid cdi_epo_espacenet_EP1709062A1
source esp@cenet
subjects CHEMISTRY
METALLURGY
ORGANIC CHEMISTRY
STEROIDS
title EXEMESTANE AND ITS INTERMEDIATES AND METHODS OF MAKING THE SAME
url https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2024-12-27T19%3A53%3A58IST&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=PASCONE,%20JOHN,%20M&rft.date=2006-10-11&rft_id=info:doi/&rft_dat=%3Cepo_EVB%3EEP1709062A1%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