http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-103012256-B

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classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D213-75
filingDate 2012-12-11-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2015-03-25-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_cff9d14d0fab6c0828b4500a4dd5b662
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publicationDate 2015-03-25-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber CN-103012256-B
titleOfInvention Method for synthesizing roflumilast
abstract The invention provides a method for synthesizing roflumilast, which comprises the following steps: (1) taking 3-cyclopropylmethoxy-4-difluoromethoxybenzoic acid for reaction to obtain 3-cyclopropylmethoxy-4-difluoromethoxybenzoyl chloride or 3-cyclopropylmethoxy-4-difluoromethoxybenzoyl bromide; (2) after the reaction in step (1) is finished, performing amidation on the resultant and 4-amino-3,5-dichloropyridine by using sodium amide as a catalyst; and (3) after the reaction is over, purifying the resultant to obtain refined roflumilast, wherein the mole ratio of sodium amide to 4-amino-3,5-dichloropyridine is greater than or equal to 1. The method uses the specific inorganic base catalyst, namely sodium amide, based on the current roflumilast synthesis process to guarantee the high purity and yield of the product and the production safety and reduce the hygroscopicity of the raw materials. Therefore, the method is more favorable for the industrial mass production.
priorityDate 2012-12-11-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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