http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2380135-T3

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filingDate 2007-11-22-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2012-05-08-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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publicationDate 2012-05-08-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber ES-2380135-T3
titleOfInvention Method of preparation of phenylalanine derivatives having quinazolinadione skeleton and intermediates for their preparation
abstract A method for preparing a phenylalanine derivative having a quinazolinadione ring represented by the following formula (1) or a pharmaceutically acceptable salt thereof, comprising the following steps (a), (b) and (c): wherein R1 represents a phenyl group that can have a substituent or a pyridyl group that can have a substituent; R2 represents an alkyl group that may have a substituent; R3 represents an alkyl group substituted with a dialkylamino group, an alkyl group substituted with a monoalkylamino group or an alkyl group substituted with an amino group; and R4 represents a hydrogen atom, an alkyl group or a benzyl group that may have a substituent; (a) reacting an acylphenylalanine derivative represented by the following formula (2) or a chemically acceptable salt thereof: in which R1 and R2 are the same as those defined above, with a reagent that introduces a carbonyl group and a derivative of anthranilic acid represented by the following formula (3) or a chemically acceptable salt thereof: in which R3 'represents an alkyl group substituted with a dialkylamino group, an alkyl group substituted with a monoalkylamino group which may have a protective group or a group alkyl substituted with an amino group which may have a protective group, to thereby form an asymmetric carboxy-urea derivative represented by the following formula (4) or a chemically acceptable salt thereof: in which R1, R2 and R3 ' no equal to those defined above; (b) converting the asymmetric carboxy-urea derivative of Formula (4) into a quinazolinadione derivative represented by the following formula (5) or a pharmaceutically acceptable salt thereof, in the presence of an agent that activates the carboxyl group: in the that from R1 to R3 'are the same as those defined above; and (c) if desired, replace an N-alkyl group with the hydrogen atom attached to the nitrogen atom present in the quinazolinadione ring of the quinazolinadione derivative of Formula (5) using an N-alkylation agent and then deprotect the resulting product, when the substituent R3 'is protected.
priorityDate 2006-11-22-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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