http://rdf.ncbi.nlm.nih.gov/pubchem/patent/NZ-613917-A
Outgoing Links
Predicate | Object |
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assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_12a9e9ce63eb0bbf3658453fb50a6d9b |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-517 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P13-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D241-38 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D239-70 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-517 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P11-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-499 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D239-86 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D239-70 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D241-38 |
filingDate | 2012-01-27-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_8b0bec8999cdbd2a3f271247b32365ea http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d5d5831d3d5fcbc940bb83a9f698dcfb http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_672c4faffce2de3ca04265364e38a87c http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_928f392e6d8d73c26f7e3aa062af68dd |
publicationDate | 2015-08-28-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | NZ-613917-A |
titleOfInvention | 9-[4-(3-chlor-2-fluor-phenylamino)-7-methoxy-quinazolin-6-yloxy]-1,4-diazaspiro[5.5]undecan-5-one dimaleate, use thereof as a drug, and production thereof |
abstract | Disclosed is crystalline 9-[4-(3-chloro-2-fluorophenylamino)-7-methoxy-quinazolin-6-yloxy]-1,4-diazaspiro[5.5]undecan-5-one dimaleate of formula (I) optionally in the form of the tautomers thereof, wherein reflections in the X-ray powder diagram occur at dhkl values of 7.11, 5.77, 4.69, 4.36, 4.15, 3.85 and 3.61 Å, and has corresponding values 2theta of 12.43, 15.33, 18.92, 20.37, 21.38, 23.06 and 24.67. Also disclosed is a process for the stereoselective preparation of the crystalline compound of formula (I) starting from 1,4-cyclohexanedione-mono-ethyleneketal. Also disclosed is a process for the chlorination of tert-butyl (trans)-9-(4-hydroxy-7-methoxy-quinazolin-6-yloxy)-5-oxo-1-(2,2,2-trifluoro-acetyl)-1,4-diaza-spiro[5.5]undecane-4-carboxylate or tert-butyl (trans)-9-(4-oxo-7-methoxy-quinazolin-6-yloxy)-5-oxo-1-(2,2,2-trifluoro-acetyl)-1,4-diaza-spiro[5.5]undecane-4-carboxylate with a reactant selected from among N-chlorosuccinimide/triphenylphosphane oxalyl chloride, thionyl chloride, phosphorus oxychloride, phosphorus pentachloride, carbon tetrachloride/triphenylphosphane, dichlorotriphenylphosphorane and P,P-dichlorophenylphosphine oxide, to form tert-butyl (trans)-9-(4-chloro-7-methoxy-quinazolin-6-yloxy)-5-oxo-1-(2,2,2-trifluoro-acetyl)-1,4-diaza-spiro[5.5]undecane-4-carboxylate. Further disclosed are intermediates such as tert-butyl (trans)-9-(3-benzyl-7-methoxy-4-oxo-3,4-dihydro-quinazolin-6-yloxy)-5-oxo-1-(2,2,2-trifluoro-acetyl)-1,4-diaza-spiro[5.5]undecane-4-carboxylate and (trans)-9-[4-(3-chloro-2-fluoro-phenylamino)-7-methoxy-quinazolin-6-yloxy]-1-(2,2,2-trifluoro-acetyl)-1,4-diaza-spiro[5.5]undecan-5-one hydrochloride. |
priorityDate | 2011-02-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 424.