http://rdf.ncbi.nlm.nih.gov/pubchem/patent/TW-200406420-A
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_8603010787905daa6f500f1cf070aff9 |
| classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/Y02P20-55 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07J73-005 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07J73-00 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07J73-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07J- |
| filingDate | 2003-07-04-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_eda82986fea77b8d594ae71ea530bede http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_21f4a556dc8878bcbd109ebe7a4488f8 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_675ff3e059858ff6e0a4e6252724817b |
| publicationDate | 2004-05-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | TW-200406420-A |
| titleOfInvention | Method for introducing a 1, 2 double bond into 3-oxo-4-azasteroid compounds |
| abstract | The invention relates to a method for producing 17β-substituted 4-aza-androst-1-ene-3-one compounds of the general formula (I) or a pharmaceutically acceptable salt thereof (in which R represents hydroxyl, optionally substituted linear or branched C1~C12 alkyl or C1~C12 alkenyl; phenyl or benzyl; a free radical-OR1, or a free radical -NHR1, or a free radical -NR1R2; R1 is hydrogen, optionally substituted linear or branched C1~C12 alkyl or C1~C12 alkenyl, or optionally substituted phenyl; R2 is hydrogenic, methyl, ethyl or propyl; or -NH1R2 represents a 5- or 6-membered heterocyclic ring), (A) introducing protective groups into the 3-keto-4-aza group of 1, 2-dihydro compound, thereby producing a compound of the general formula (III) (in which R3 represents trialkyl silyl, or together with R4 represent the following free radical -C(O)-C(O)- or -C(O)-Y-C(O)-; R4 represents alkyoxylcarbonyl or phenoxycarbonyl, and preferably Boc(Boc=ter-butyloxycarbonyl, or trialkylsilyl, or together with R3 represent the following free radical: -C(O)-C(O)- or -C(O)-Y-C(O)-Y-[(R5)(R6)]-, or -CH(R5)=CH(R5)-, or o-phenyl alkene; R5 and R6 independently represent hydrogenic, linear or branched C1~C8 alkyl or alkenyl, and optionally substituted phenyl or benzyl; and n is an 1~4 integer; in which, when R represents hydroxyl, optionally R has been reacted with a protective group); (B) reacting the obtained compound so obtained in the presence of (i) a dehydration catalyst; and (ii) optionally substituted benzoquinone, allylethylcarbonate and/or allylpropylcarbonate; and, (C) removing the protective groups R3 and R4 and converting the resulting compound to a salt if necessary. |
| priorityDate | 2002-07-16-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
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