http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2371369-T3
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_966a6c1f382ec9bcb5e3839dfd73e5b8 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D455-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C59-31 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-04 |
| filingDate | 2007-09-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2011-12-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_17ceb5bc63c44b3ab4d53b3ebf35a1d6 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_366ae3c2a0ea1a3ba1e036904c9b0ff8 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_865a336823c15f176b5971c068317185 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_54989d1392e896857319092e69f8d3cc |
| publicationDate | 2011-12-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | ES-2371369-T3 |
| titleOfInvention | PROCEDURE FOR THE PREPARATION OF DERIVATIVES PIRIDO [2,1-A] ISOQUINOLINA, WHICH INCLUDES THE OPTICAL RESOLUTION OF AN ENAMINE. |
| abstract | Process for the preparation of pyrido [2,1-a] isoquinoline derivatives of the formula: wherein R 2, R 3 and R 4 are each independently selected from the group consisting of hydrogen, halogen, hydroxy, alkyl C1-C6, C1-C6 alkoxy and C1-C6 alkenyl, wherein C1-C6 alkyl, C1-C6 alkoxy and C1-C6 alkenyl may optionally be substituted with a group selected from C1-C6 alkoxycarbonyl, aryl and heterocyclyl, comprising one or more of steps a), b), c) or d), in which a) comprises the optical resolution of an enamine of the formula: wherein R 2, R 3 and R 4 are as defined above , and R 1 is C 1 -C 6 alkyl or benzyl, in the presence of an optically active optical resolution agent, forming the salt (S) -enamine of the formula: wherein R 1, R 2, R 3 and R 4 are such as defined above, and RCO2 is the conjugate base of the resolution agent; step b) comprises the transformation of the salt (S) -enamine of formula III into the ester of formula: wherein R 1, R 2, R 3 and R 4 are as indicated above and "Prot" is refers to an amino protecting group; step c) comprises amidation of the ester of formula IV to form the amide of formula: wherein R 2, R 3, R 4 and Prot are as defined above, and step d) comprises degradation of the amide of formula V to form the amine of formula: wherein R 2, R 3, R 4 and Prot are as defined above, in which the process comprises step a), and in which the process is characterized in that the optical resolution in step a) is a dynamic resolution induced by crystallization. |
| priorityDate | 2006-09-15-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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