http://rdf.ncbi.nlm.nih.gov/pubchem/patent/NZ-576034-A
Outgoing Links
Predicate | Object |
---|---|
assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_0a555bd18827bb277757c67b9086d8ba |
classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07B2200-13 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/Y02P20-55 |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-445 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D211-54 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-445 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P31-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D211-54 |
filingDate | 2007-10-03-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_706249ba8adf0db4c3f2d172990f59fa http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9b294e71d5c684daa2bce1592c9bd80b http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_797abecf2b513a905a0eff46f1f5eed2 |
publicationDate | 2011-07-29-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | NZ-576034-A |
titleOfInvention | Process for the preparation of pleuromutilins |
abstract | Disclosed is a process for the preparation of piperidinylsulfanylacetylmutilins of formula I wherein the carbon atom of the piperidine ring attached to the sulphur atom is either in the (S)-configuration or in the (R)-configuration and the 2-amino-3-methyl-butyryl group attached to the piperidine ring is either in the (S)-configuration or in the (R)-configuration, comprising the steps of: a) deprotecting an N-protected piperidinylsulfanylacetylmutilin of formula II and isolating a compound of formula III wherein the carbon atom Of the piperidine ring attached to the sulphur atom is either in the (S)-configuration or in the (R)-configuration, in free form or in the form of an acid addition salt, in crystalline form, b) acylating said compound of formula III with either (R)- or (S)-valine protected as an enamine and activated as a carbonic acid mixed anhydride to form a compound of formula VI wherein R1 and R2 are C1-4 alkyl, and R, is hydrogen or C1-4 alkyl, deprotecting the compound of formula IV and isolating the compound of formula I. Also disclosed is a compound of formula (IV); the acid salt of formula (III) in crystalline form; 14-O-[(N-3-methyI-2-(R)-amino-butyryl-piperidine-3(S)- yl)sulfanyl)acetyl]mutilin hydrochloride; and a pharmaceutical composition containing crystalline 14-O-[(N-3-methyI-2-(R)-amino-butyryl-piperidine-3(S)- yl)sulfanyl)acetyl]mutilin hydrochloride |
priorityDate | 2006-10-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 81.