http://rdf.ncbi.nlm.nih.gov/pubchem/patent/TW-201026704-A

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assignee http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_870eb0bfda8e9252517b2b7ae44506e0
classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-00
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C233-33
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4439
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-495
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C231-12
classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C233-07
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-04
filingDate 2010-01-12-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_806cde51624285fafbde711d79e42b99
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_942ae5a801facd924490c33c801934d8
publicationDate 2010-07-16-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber TW-201026704-A
titleOfInvention Process for the preparation of N-[5-(3-dimethylamino-acryloyl)-2-fluoro-phenyl]-N-methyl-acetamide
abstract The present invention relates to a new process for the preparation of N-[5-(3-dimethylamino-acryloyl)-2-fluoro-phenyl]-N-methyl-acetamide (I) in a high yield and high purity, which is an intermediate in the synthesis of compounds with affinity for GABA<sub>A</sub> receptor. In this process, N-(5-acetyl-2-fluorophenyl)-N-methyl-acetamide (VI) is reacted with an excess of N,N-dimethylformamide dimethyl acetal (NNDMF-DMA). The present invention also provides a new process for the preparation of a compound with affinity for GABA<sub>A</sub> receptor, N-{2-fluoro-5-[3-(thiophene)-2-carbonyl-pyrazolo[1,5-a]pyrimidin-7-yl]phenyl}-N-methyl-acetamide (II), which comprises the following steps: (a) methylation of N-(5-acetyl-2-fluorophenyl)-N-acetamide (IV) with a methyl sulfonate, (b) reaction of the resulting compound (VI) with NNDMF-DMA, and c reaction of the resulting compound (I) with (5-amino-1H-pirazol-4-yl) thiophen-2-yl-methanone (III) in glacial acetic acid. The present invention also relates to new intermediate (VI).
priorityDate 2009-01-13-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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