http://rdf.ncbi.nlm.nih.gov/pubchem/patent/RO-85987-B1

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classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D205-08
filingDate 1981-02-06-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_74974016bdd4a69c46a6c609539f1462
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_fe632cda1f8a125553fb6a9504b37e34
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publicationDate 1985-01-30-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber RO-85987-B1
titleOfInvention PROCESS FOR THE PREPARATION OF LACTAMES
abstract The invention relates to a process for the preparation of lactams of general formula I wherein R1 represents a phenylacetyl group or a protecting group selected from benzyloxycarbonyl or t-butoxycarbonyl, one of R2 and R3 represents hydrogen and the other hydrogen or lower alkyl and M @ + represents a tetraalkylammonium cation, characterized in that a compound of the general formula (II): wherein R1, R2 and R3 are as defined above and M5 is a leaving group of mesylate, is sulfonated by treatment with chlorosulfonic acid in the presence of 2-methylpyridine at reflux temperature in a halogenated aliphatic hydrocarbon solvent, followed by the addition of tetra-n-butylammonium acid sulphate with the intermediate compound of formula III: (see formula) wherein R 1, R 2, R 3, Ms and M 1a + have the above-mentioned meaning, which is cyclized by treatment with a base selected from an alkali metal carbonate or bicarbonate in an amest e. g. water and a halogenated aliphatic hydrocarbon as the solvent at reflux temperature, then from the compounds of general formula I obtained, the protecting group is removed to obtain a compound wherein R1 is hydrogen and optionally converts the salts of formula I into free acids by methods known per se.
priorityDate 1981-02-06-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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Total number of triples: 34.