http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-0330625-A3

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filingDate 1989-02-16-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 1991-09-18-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber EP-0330625-A3
titleOfInvention Total synthesis method for making an indole structure derivative product class, of the triptamine type, in particular, melatonin or N-acetyl-5-methoxytriptamine type, having a high purity degree and easily soluble, for therapeutic use against acquired immuno-deficiency syndromes
abstract The present invention relates to : n 1) a method for the total synthesis of an indole struc­nture derivative product class,of the triptamine type, nin particular of the melatonine or N-Acetyl-5-Methoxy-­ntriptamine type; 2) the use of melatonine or N-acetyl-5-methoxytriptamine nas a drug with doses from 2 mg to 20 mg per day,in an noral,intramuscolar or endovenous way; 3) the use of melatonine or N-acetyl-5-methoxytriptamine, nin combination with an azidothymidine treating process, nin order to improve the curative effects. n The subject total synthesis process consists of ncombining potassium phthalamide and di-bromopropane in norder to obtain 3-bromopropylphthalamide;adding, in the npresence of ethanol dissolved sodium,acetacetic esther nin order to obtain ethyl-2-acetyl-5-phthalimido-penta­n n nnoate ;adding diazo-p-anisidine so as to obtain 2-­ncarboxyethyl-3-(2-phthalimidoethyl)-5-methoxy-indole. n The main feature of the invention is that nto the 2-carboxyethyl-3-(2-phthalimidoethyl)-5-methoxy­n-indole there are added NaOH 2N and 20% H₂SO₄ in order nto obtain raw 5-methoxytriptamine;which is purified by nmeans of hexamethyldisilazane,with the formation of the nrelated mono and bi-derivative therefrom there is obtain­ned the starting product which is purified by means of naqueous methanol. n The subject method,in particular,is specifically ndesigned for provided high purity melatonine,or N-acetyl-­n5-methoxytriptamine,with a great yield,which is water nsoluble and may be used for therapeutic purposes. n The thus obtained melatonine,has such a purity that nit can be used,in suitable packages,both in tumoral nphrophilaxy and tumoral terapy,as well as against the nacquired immuno-deficiency syndromes,o so called AIDS.
priorityDate 1988-02-25-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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Total number of triples: 42.