http://rdf.ncbi.nlm.nih.gov/pubchem/patent/WO-2014180271-A1

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classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-12
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classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D405-12
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D307-20
filingDate 2014-04-30-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c167d6630cce17b679d6ef6213023042
publicationDate 2014-11-13-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber WO-2014180271-A1
titleOfInvention Method for preparing afatinib and intermediate thereof
abstract Revealed in the present invention is a method for preparing Afatinib (I): using 2-nitrile-4-[4-(N,N-dimethylamino)-1-oxo-2-buten-1-yl]amino-5-[(S)- (tetrahydrofuran-3-yl)oxy]aniline (II) and 4-fluoro-3-chloroaniline (III) as starting materials, and respectively performing a condensation and cyclization reaction with N,N-dimethylformamide dimethyl acetal (IV) to prepare Afatinib (I), wherein the method significantly reduces the manufacturing steps of Afatinib and greatly lower the costs. In addition, also provided in the present invention is a method for preparing an intermediate of Afatinib, wherein the method has a stable process, uses readily available starting materials, has a low cost, and all the reactions are classic reactions, suitable for meeting amplification requirements in the industry.
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priorityDate 2013-05-10-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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