75648-24-7Relevant academic research and scientific papers
Synthesis of 2-[18F]Fluoro-2-deoxyisosorbide 5-mononitrate and Assessment of Its in vivo Biodistribution as Determined by Dynamic Positron Emission Tomography (PET)
Santschi, Nico,Wagner, Stefan,Daniliuc, Constantin,Hermann, Sven,Sch?fers, Michael,Gilmour, Ryan
, p. 1724 - 1732 (2015)
Herein we disclose the synthesis of 2-fluoro-2-deoxyisosorbide 5-mononitrate (2F-IS-5MN), a fluorinated analogue of the commonly prescribed vasodilator isosorbide 5-mononitrate (IS-5MN). X-ray structural data for IS-5MN and its C2-epimeric congener IM-5MN are presented together with structural data for 2F-IS-5MN. Radioisotope labeling of 2F-IS-5MN has, for the first time, allowed observation of the in vivo biodistribution of this organic nitrate by means of dynamic positron emission tomography (PET) in wild-type mice. Visualization breakthrough: Herein we disclose the synthesis of a fluorinated analogue of the commonly prescribed vasodilator isosorbide 5-mononitrate (IS-5MN). Radioisotope labeling of 2F- IS-5MN has, for the first time, allowed observation of the in vivo biodistribution of this organic nitrate by means of dynamic positron emission tomography (PET) in wild-type mice.
COMPOUNDS AND COMPOSITIONS FOR USE IN TREATING PSORIASIS
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Paragraph 0095, (2018/10/19)
Compounds and pharmaceutical compositions for use in the treatment of psoriasis are disclosed. Preferred compounds have demonstrated efficacy in reducing skin scaling, erythema and skin thickness in the mouse model of Aldara-induced psoriasis.
Process for selectively producing isosorbide-5-nitrate
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, (2008/06/13)
The present invention is related to a new process for selectively preparing isosorbide-5-nitrate (1.4-3.6-dianhydrosorbitol-5-nitrate) by subjecting isomannide (1.4-3.6-dianhydromannitol) in an organic solvent or an aqueous-organic reaction medium to reaction with the equivalent amount of an acid halogenide or the anhydride of a benzene or naphthalene sulfonic acid possibly substituted by lower alkyl, lower alkoxy and/or halogen, of a perfluoro - lower alkane-sulfonic acid, of a lower alkanesulfonic acid or of a perfluoro - lower - alkanoic acid or with the equivalent amount of an acid halogenide of a carbamic acid or of sulphurous acid; subjecting the resulting isomannide-2-ester in the presence of a solvent and possibly with heating, to reaction with an alkali metal salt or an ammonium salt of a benzoic acid possibly substituted by lower alkyl, lower alkoxy and/or halogen or of a lower alkanoic acid; converting the hydroxy group in the 5-position of the resulting isosorbide-2-ester into the nitric acid ester group in manners known per se by reaction with nitric acid; and subjecting the resulting isosorbide-2-ester-5-nitrate to selective hydrolysis and/or reesterification in an organic or aqueous-organic solvent with an alkali metal hydroxide in manners known per se.
