FREMGANGSMAATE FOR FREMSTILLING AV OPTISK RENT S-3-MORFOLINO-4-(3'-TERTBUTYLAMINO-2'-HYDROXYPROPOXY)-1,2,5-THIADIAZOL
The novel dialkanoyl, diaroyl or alkanoyl-aroyl L-tartaric acid-O-monoesters of 3-morpholino-4-(3'-tert-butylamino-2'-hydroxypropoxy)-1,2,5-thiadiazol e correspond to the formula (R = the alkyl or aryl group). They are intermediates in the preparation of S-3-morpholino-4-(3'-tert-buty...
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creator | HIETANIEMI, LAURI NUPPONEN, HEIKKI |
description | The novel dialkanoyl, diaroyl or alkanoyl-aroyl L-tartaric acid-O-monoesters of 3-morpholino-4-(3'-tert-butylamino-2'-hydroxypropoxy)-1,2,5-thiadiazol e correspond to the formula (R = the alkyl or aryl group). They are intermediates in the preparation of S-3-morpholino-4-(3'-tert-butylamino-2'-hydroxypropoxy)-1,2,5-thiadiaz ole, i.e. of S-timolol, which has useful beta -blocking activity, as well as of its acid addition salts. The said L-tartaric acid-O-monoesters are prepared from the corresponding L-tartaric anhydride and R,S-timolol, and their resolution is carried out by crystallising the racemic ester from an alcohol or from a mixture of alcohol and water in a pH range from 7 to 2, resulting in the isolation of the L-tartaric acid-O-monoester of S-timolol in optically pure form, from which ester S-timolol is liberated by acid hydrolysis and can be converted to the desired acid salt. |
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They are intermediates in the preparation of S-3-morpholino-4-(3'-tert-butylamino-2'-hydroxypropoxy)-1,2,5-thiadiaz ole, i.e. of S-timolol, which has useful beta -blocking activity, as well as of its acid addition salts. The said L-tartaric acid-O-monoesters are prepared from the corresponding L-tartaric anhydride and R,S-timolol, and their resolution is carried out by crystallising the racemic ester from an alcohol or from a mixture of alcohol and water in a pH range from 7 to 2, resulting in the isolation of the L-tartaric acid-O-monoester of S-timolol in optically pure form, from which ester S-timolol is liberated by acid hydrolysis and can be converted to the desired acid salt.</description><edition>4</edition><language>nor</language><subject>CHEMISTRY ; HETEROCYCLIC COMPOUNDS ; METALLURGY ; ORGANIC CHEMISTRY</subject><creationdate>1988</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&date=19880321&DB=EPODOC&CC=NO&NR=158020B$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,777,882,25545,76296</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=19880321&DB=EPODOC&CC=NO&NR=158020B$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>HIETANIEMI, LAURI</creatorcontrib><creatorcontrib>NUPPONEN, HEIKKI</creatorcontrib><title>FREMGANGSMAATE FOR FREMSTILLING AV OPTISK RENT S-3-MORFOLINO-4-(3'-TERTBUTYLAMINO-2'-HYDROXYPROPOXY)-1,2,5-THIADIAZOL</title><description>The novel dialkanoyl, diaroyl or alkanoyl-aroyl L-tartaric acid-O-monoesters of 3-morpholino-4-(3'-tert-butylamino-2'-hydroxypropoxy)-1,2,5-thiadiazol e correspond to the formula (R = the alkyl or aryl group). They are intermediates in the preparation of S-3-morpholino-4-(3'-tert-butylamino-2'-hydroxypropoxy)-1,2,5-thiadiaz ole, i.e. of S-timolol, which has useful beta -blocking activity, as well as of its acid addition salts. The said L-tartaric acid-O-monoesters are prepared from the corresponding L-tartaric anhydride and R,S-timolol, and their resolution is carried out by crystallising the racemic ester from an alcohol or from a mixture of alcohol and water in a pH range from 7 to 2, resulting in the isolation of the L-tartaric acid-O-monoester of S-timolol in optically pure form, from which ester S-timolol is liberated by acid hydrolysis and can be converted to the desired acid salt.</description><subject>CHEMISTRY</subject><subject>HETEROCYCLIC COMPOUNDS</subject><subject>METALLURGY</subject><subject>ORGANIC CHEMISTRY</subject><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>1988</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNqFik0LgkAUAL10iOo3tDcLfOBHQtc1d3VJfbL7iuwiEtspSrD-fwrdOw3MzNz5SC3KjFeZKTknwSRqNilDqihUlTF-ZliTMkemRUXMQAQlaoljRNjBJnKBhKbkRE3By0mGLuRNqvHS1BrrEVsIvNCLgXLFU8WvWCyd2b17DHb148JZS0GHHGz_au3Qdzf7tO-2wiDe-6GfJNH_4wvzyjg1</recordid><startdate>19880321</startdate><enddate>19880321</enddate><creator>HIETANIEMI, LAURI</creator><creator>NUPPONEN, HEIKKI</creator><scope>EVB</scope></search><sort><creationdate>19880321</creationdate><title>FREMGANGSMAATE FOR FREMSTILLING AV OPTISK RENT S-3-MORFOLINO-4-(3'-TERTBUTYLAMINO-2'-HYDROXYPROPOXY)-1,2,5-THIADIAZOL</title><author>HIETANIEMI, LAURI ; NUPPONEN, HEIKKI</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_NO158020BB3</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>nor</language><creationdate>1988</creationdate><topic>CHEMISTRY</topic><topic>HETEROCYCLIC COMPOUNDS</topic><topic>METALLURGY</topic><topic>ORGANIC CHEMISTRY</topic><toplevel>online_resources</toplevel><creatorcontrib>HIETANIEMI, LAURI</creatorcontrib><creatorcontrib>NUPPONEN, HEIKKI</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>HIETANIEMI, LAURI</au><au>NUPPONEN, HEIKKI</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>FREMGANGSMAATE FOR FREMSTILLING AV OPTISK RENT S-3-MORFOLINO-4-(3'-TERTBUTYLAMINO-2'-HYDROXYPROPOXY)-1,2,5-THIADIAZOL</title><date>1988-03-21</date><risdate>1988</risdate><abstract>The novel dialkanoyl, diaroyl or alkanoyl-aroyl L-tartaric acid-O-monoesters of 3-morpholino-4-(3'-tert-butylamino-2'-hydroxypropoxy)-1,2,5-thiadiazol e correspond to the formula (R = the alkyl or aryl group). They are intermediates in the preparation of S-3-morpholino-4-(3'-tert-butylamino-2'-hydroxypropoxy)-1,2,5-thiadiaz ole, i.e. of S-timolol, which has useful beta -blocking activity, as well as of its acid addition salts. The said L-tartaric acid-O-monoesters are prepared from the corresponding L-tartaric anhydride and R,S-timolol, and their resolution is carried out by crystallising the racemic ester from an alcohol or from a mixture of alcohol and water in a pH range from 7 to 2, resulting in the isolation of the L-tartaric acid-O-monoester of S-timolol in optically pure form, from which ester S-timolol is liberated by acid hydrolysis and can be converted to the desired acid salt.</abstract><edition>4</edition><oa>free_for_read</oa></addata></record> |
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subjects | CHEMISTRY HETEROCYCLIC COMPOUNDS METALLURGY ORGANIC CHEMISTRY |
title | FREMGANGSMAATE FOR FREMSTILLING AV OPTISK RENT S-3-MORFOLINO-4-(3'-TERTBUTYLAMINO-2'-HYDROXYPROPOXY)-1,2,5-THIADIAZOL |
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