http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-1266898-A4

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filingDate 2001-02-27-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ed70aba4a5dc18552727935a769ecb56
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publicationDate 2003-05-21-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber EP-1266898-A4
titleOfInvention PROCESSES FOR PRODUCING THIENOPYRAMIDINE DERIVATIVES
abstract Processes for mass-producing on an industrial scale intermediates for the preparation of thienopyrimidine derivatives exhibiting GnRH antagonism, and so on. Specifically, a process for the production of compounds of the general formula (III) or salts thereof (wherein R1 is hydrogen, nitro, halogeno, phthalimido, mono- or di-(alkylcarbonyl)amino, or alkoxy; and R2 is alkyl or aryl), which comprises converting a compound of the general formula (I) or a salt thereof: into an acid halide corresponding thereto, reacting this acid halide with a malonic ester and a magnesium alkoxide, treating the obtained product with an acid, and reacting the resulting product with sulfur and a compound of the general formula: NCCH¿2COOR?2 or a salt thereof in the presence of a primary amine. The processes make it possible to mass-produce thienopyrimidine derivatives exhibiting GnRH antagonism in high yield at high efficiency on an industrial scale by simple means.
priorityDate 2000-02-29-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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