http://rdf.ncbi.nlm.nih.gov/pubchem/patent/IE-893623-L

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assignee http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_49d10e350f03a5e0edcba0f3cd3480c0
classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-505
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D475-04
classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D475-04
filingDate 1989-11-10-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 1990-05-11-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber IE-893623-L
titleOfInvention Method for the preparation of tetrahydrofolates
abstract The invention relates to a process for the separation of (6R,S)-folinates into their diastereomers, which comprises mixing an aqueous solution of a salt of (6R,S)-folinic acid with a water-soluble alkali metal, ammonium or alkaline earth metal salt of an inorganic or organic acid, removing the salt which separates out and which predominantly consists of the appropriate (6R)-folinate by filtration, and isolating the desired (6S)-folinate from the filtrate. <??>The process for the isolation of (6S)-folinate comprises causing the appropriate (6S)-folinate to separate out of the said filtrate by adding a water-miscible organic solvent and/or preferably a water- soluble alkaline earth metal salt, filtering it off and removing remaining (6R)-folinate by recrystallisation. <??>The separation off of alkaline earth metal salts of (6R)-folinic acid is preferably carried out at approximately neutral pH. <??>The alkali metal or alkaline earth metal salt of (6R,S)-folinic acid which is preferably used is the sodium, calcium or magnesium salt, the water-soluble alkali metal or ammonium salt of inorganic acids is preferably a sodium, potassium or ammonium halide, especially sodium iodide, sodium bromide, sodium chloride, potassium iodide, potassium bromide, potassium chloride, ammonium iodide, ammonium bromide or ammonium chloride, and the organic solvent for separating out the appropriate (6S)-folinate is a lower alcohol or a lower ketone, and the water-soluble alkaline earth metal salt is a calcium or magnesium halide. <??>The resulting (6S)-folinates are valuable medicaments for the treatment of megaloblastic folic acid deficiency anaemia, as antidote for enhancing the tolerability of folic acid antagonists, specifically of aminopterin, methotrexate and 5-fluorouracil in cancer therapy (leucovorin rescue) and the treatment of autoimmune diseases such as psoriasis and rheumatoid arthritis and for enhancing the tolerability of certain antiparasitics. n[EP0367902A2]
priorityDate 1988-11-11-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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