http://rdf.ncbi.nlm.nih.gov/pubchem/patent/IL-134975-A
Outgoing Links
Predicate | Object |
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assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_c7e02134f8e73be58f71c75e4b0c4a3b |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D457-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D- http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07F7-10 |
filingDate | 2000-03-09-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationDate | 2004-06-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | IL-134975-A |
titleOfInvention | Process for producing cabergoline and related compounds and novel intermediates therefor |
abstract | A process for the preparation of a compound of the formula including stereoisomers as well as acid addition salts thereof, wherein R1 is selected from alkyl having from 1 to 4 carbon atoms, cyclohexyl, phenyl, and dimethylamino alkyl group -(CH2)nNMe2 in which n is an integer from 1 to 8, R2 is selected from hydrogen, alkyl having from 1 to 4 carbon atoms, cyclohexyl, phenyl, dimethylamino alkyl group -(CH2)nNMe2 in which n is an integer from 1 to 8, pyridyl, pyrimidyl, pyrazinyl, pyridazinyl, thiazolyl or thiadiazolyl, R3 represents a hydrocarbon group having from 1 to 4 carbon atoms, and R4 is selected from hydrogen, halogen, methylthio and phenylthio group; which process comprises silylating with a silylation agent a compound of the formula 1074 י" ב בסיון התשס" ד - June 1, 2004 including stereoisomers as well as metal or ammonium salts or acid addition salts thereof, wherein R2, R3 and R4 are as defined above, and reacting the resultant product with a compound of the formula R1-N=C=O wherein R1 is as defined above, followed by desilylation. Claimed as new are compounds of the formula including stereoisomers as well as acid addition salts thereof, wherein R2 is selected from hydrogen, alkyl having from 1 to 4 carbon atoms, cyclohexyl, phenyl, dimethylamino alkyl group -(CH2)nNMe2 in which n is an integer from 1 to 8, pyridyl, pyrimidyl, pyrazinyl, pyridazinyl, thiazolyl or thiadiazolyl, R3 represents a hydrocarbon group having from 1 to 4 carbon atoms, and R4 is selected from hydrogen, halogen, methylthio and phenylthio group; and R6, R7 and R8 may be the same or different and are selected from the group consisting of alkyl having from 1 to 4 carbon atoms, aryl and aralkyl radicals and crystalline cabergoline which exhibits an IR spectrum substantially as shown in Fig. 1 and DSC pattern substantially as shown in Fig. 2 as given in the specification. 1075 י" ב בסיון התשס" ד - June 1, 2004 |
priorityDate | 2000-03-09-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 141.