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Water soluble derivatives of taxol

dc.contributor.assigneeVirginia Tech Intellectual Properties, Inc.en
dc.contributor.inventorKingston, David G. I.en
dc.contributor.inventorZhao, Zhi-Yangen
dc.date.accessed2016-08-19en
dc.date.accessioned2016-08-24T17:55:39Zen
dc.date.available2016-08-24T17:55:39Zen
dc.date.filed1991-05-01en
dc.date.issued1994-10-04en
dc.description.abstractSulfonated 2'-acryloyltaxol and sulfonated 2'-O-acyl acid taxol derivatives are synthesized which have improved water solubility and stability while maintaining bio-activity. In particular, 2'-[(3-sulfo-1-oxopropyl)oxy]taxol sodium salt is synthesized by reacting taxol with acrylic acid, and subsequently reacting the 2'-acryloyltaxol with bisulfite in a Michael reaction. 2'-{[4-((2-sulfoethyl)amino)-l,4-dioxobutyl]oxy} taxol sodium salt and 2'-{[4-((3-sulfopropyl)amino)-1,4-dioxobutyl]oxy} taxol sodium salt are synthesized by reacting 2'-succinyltaxol with the tetrabutylammonium salts of taurine and 3-aminopropyl sulfonic acid, respectively, and subsequently exchanging the ammonium with sodium. Glycol derivatives of 2'-O-acyl acid taxols with improved water solubility are synthesized by reaction of a glycol with 2'-O-acyl acid taxol.en
dc.format.mimetypeapplication/pdfen
dc.identifier.applicationnumber7694077en
dc.identifier.patentnumber5352805en
dc.identifier.urihttp://hdl.handle.net/10919/72821en
dc.identifier.urlhttp://pimg-fpiw.uspto.gov/fdd/05/528/053/0.pdfen
dc.language.isoen_USen
dc.publisherUnited States Patent and Trademark Officeen
dc.subject.cpcC07D305/14en
dc.subject.uspc549/510en
dc.subject.uspcother549/511en
dc.titleWater soluble derivatives of taxolen
dc.typePatenten
dc.type.dcmitypeTexten
dc.type.patenttypeutilityen

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