OPTICALLY ACTIVE PIPERIDINE DERIVATIVE ACID ADDITION SALT AND ITS PRODUCTION
PROBLEM TO BE SOLVED: To obtain the subject new compound excellent in antihistaminic activity and antiallergic activity, having a few hygroscopic property, excellent in physicochemical property and useful as a medicine. SOLUTION: This new compound is benzenesulfonic acid salt of a compound represent...
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| creator | FUJIWARA HIROSHI KITA JUNICHIRO TAKAMURA SHINJI |
| description | PROBLEM TO BE SOLVED: To obtain the subject new compound excellent in antihistaminic activity and antiallergic activity, having a few hygroscopic property, excellent in physicochemical property and useful as a medicine. SOLUTION: This new compound is benzenesulfonic acid salt of a compound represented by formula I. The new compound is preferably obtained by subjecting 1 mol compound of formula I to salt formation reaction with 0.9-1.2 mol benzenesulfonic acid in a solvent such as ethyl acetate, preferably at 10-35 deg.C. The solvent is preferably used in an amount of 1 to 10 L based on 1 mol compound of formula I. The temperature at salt deposition is preferably -10 to 15 deg.C. The compound of formula I is obtained by reacting an optically active (S)-4-[(4-chlorophenyl) (2-pyridyl)methoxy]piperidin with a compound of formula II (W is an eleiminable group; R is a lower alkyl) (e.g. ethyl 4- bromobutanoate) in an inert solvent in the presence of a base and then subjecting the resultant compound of formula III to hydrolysis reaction. |
| format | Patent |
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SOLUTION: This new compound is benzenesulfonic acid salt of a compound represented by formula I. The new compound is preferably obtained by subjecting 1 mol compound of formula I to salt formation reaction with 0.9-1.2 mol benzenesulfonic acid in a solvent such as ethyl acetate, preferably at 10-35 deg.C. The solvent is preferably used in an amount of 1 to 10 L based on 1 mol compound of formula I. The temperature at salt deposition is preferably -10 to 15 deg.C. The compound of formula I is obtained by reacting an optically active (S)-4-[(4-chlorophenyl) (2-pyridyl)methoxy]piperidin with a compound of formula II (W is an eleiminable group; R is a lower alkyl) (e.g. ethyl 4- bromobutanoate) in an inert solvent in the presence of a base and then subjecting the resultant compound of formula III to hydrolysis reaction.</description><edition>7</edition><language>eng</language><subject>CHEMISTRY ; HETEROCYCLIC COMPOUNDS ; HUMAN NECESSITIES ; HYGIENE ; MEDICAL OR VETERINARY SCIENCE ; METALLURGY ; ORGANIC CHEMISTRY ; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES ; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</subject><creationdate>2000</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=20000718&DB=EPODOC&CC=JP&NR=2000198784A$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,777,882,25545,76296</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20000718&DB=EPODOC&CC=JP&NR=2000198784A$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>FUJIWARA HIROSHI</creatorcontrib><creatorcontrib>KITA JUNICHIRO</creatorcontrib><creatorcontrib>TAKAMURA SHINJI</creatorcontrib><title>OPTICALLY ACTIVE PIPERIDINE DERIVATIVE ACID ADDITION SALT AND ITS PRODUCTION</title><description>PROBLEM TO BE SOLVED: To obtain the subject new compound excellent in antihistaminic activity and antiallergic activity, having a few hygroscopic property, excellent in physicochemical property and useful as a medicine. SOLUTION: This new compound is benzenesulfonic acid salt of a compound represented by formula I. The new compound is preferably obtained by subjecting 1 mol compound of formula I to salt formation reaction with 0.9-1.2 mol benzenesulfonic acid in a solvent such as ethyl acetate, preferably at 10-35 deg.C. The solvent is preferably used in an amount of 1 to 10 L based on 1 mol compound of formula I. The temperature at salt deposition is preferably -10 to 15 deg.C. The compound of formula I is obtained by reacting an optically active (S)-4-[(4-chlorophenyl) (2-pyridyl)methoxy]piperidin with a compound of formula II (W is an eleiminable group; R is a lower alkyl) (e.g. ethyl 4- bromobutanoate) in an inert solvent in the presence of a base and then subjecting the resultant compound of formula III to hydrolysis reaction.</description><subject>CHEMISTRY</subject><subject>HETEROCYCLIC COMPOUNDS</subject><subject>HUMAN NECESSITIES</subject><subject>HYGIENE</subject><subject>MEDICAL OR VETERINARY SCIENCE</subject><subject>METALLURGY</subject><subject>ORGANIC CHEMISTRY</subject><subject>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</subject><subject>SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</subject><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>2000</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNrjZPDxDwjxdHb08YlUcHQO8QxzVQjwDHAN8nTx9HNVcAEywhzBoo7Oni4Kji4uniGe_n4KwY4-IQqOfi4KniHBCgFB_i6hziBxHgbWtMSc4lReKM3NoOTmGuLsoZtakB-fWlyQmJyal1oS7xVgZGBgYGhpYW5h4mhMlCIAHMkueQ</recordid><startdate>20000718</startdate><enddate>20000718</enddate><creator>FUJIWARA HIROSHI</creator><creator>KITA JUNICHIRO</creator><creator>TAKAMURA SHINJI</creator><scope>EVB</scope></search><sort><creationdate>20000718</creationdate><title>OPTICALLY ACTIVE PIPERIDINE DERIVATIVE ACID ADDITION SALT AND ITS PRODUCTION</title><author>FUJIWARA HIROSHI ; KITA JUNICHIRO ; TAKAMURA SHINJI</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_JP2000198784A3</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng</language><creationdate>2000</creationdate><topic>CHEMISTRY</topic><topic>HETEROCYCLIC COMPOUNDS</topic><topic>HUMAN NECESSITIES</topic><topic>HYGIENE</topic><topic>MEDICAL OR VETERINARY SCIENCE</topic><topic>METALLURGY</topic><topic>ORGANIC CHEMISTRY</topic><topic>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</topic><topic>SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</topic><toplevel>online_resources</toplevel><creatorcontrib>FUJIWARA HIROSHI</creatorcontrib><creatorcontrib>KITA JUNICHIRO</creatorcontrib><creatorcontrib>TAKAMURA SHINJI</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>FUJIWARA HIROSHI</au><au>KITA JUNICHIRO</au><au>TAKAMURA SHINJI</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>OPTICALLY ACTIVE PIPERIDINE DERIVATIVE ACID ADDITION SALT AND ITS PRODUCTION</title><date>2000-07-18</date><risdate>2000</risdate><abstract>PROBLEM TO BE SOLVED: To obtain the subject new compound excellent in antihistaminic activity and antiallergic activity, having a few hygroscopic property, excellent in physicochemical property and useful as a medicine. SOLUTION: This new compound is benzenesulfonic acid salt of a compound represented by formula I. The new compound is preferably obtained by subjecting 1 mol compound of formula I to salt formation reaction with 0.9-1.2 mol benzenesulfonic acid in a solvent such as ethyl acetate, preferably at 10-35 deg.C. The solvent is preferably used in an amount of 1 to 10 L based on 1 mol compound of formula I. The temperature at salt deposition is preferably -10 to 15 deg.C. The compound of formula I is obtained by reacting an optically active (S)-4-[(4-chlorophenyl) (2-pyridyl)methoxy]piperidin with a compound of formula II (W is an eleiminable group; R is a lower alkyl) (e.g. ethyl 4- bromobutanoate) in an inert solvent in the presence of a base and then subjecting the resultant compound of formula III to hydrolysis reaction.</abstract><edition>7</edition><oa>free_for_read</oa></addata></record> |
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| subjects | CHEMISTRY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS |
| title | OPTICALLY ACTIVE PIPERIDINE DERIVATIVE ACID ADDITION SALT AND ITS PRODUCTION |
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