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classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D233-22
classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D233-22
filingDate 2020-06-19-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2022-10-04-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_71131fdef8bc7d767faadc93a08e40bd
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ce256cc605b614c596b06086230113a1
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_600c3325cf6f84134431d08fb41a219d
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_96758df7c9ade0d5590915d87e44d113
publicationDate 2022-10-04-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber US-11459303-B2
titleOfInvention Process for the synthesis of lofexidine
abstract Disclosed is a process for the synthesis of lofexidine of formula (I) and the hydrochloride salt thereof (II), from ethyl 2-(2,6-dichlorophenoxy)propionate (III) and ethylenediamine in the presence of tetravalent titanium alkoxides, preferably titanium isopropoxide, in an apolar solvent such as toluene. A further object of the present invention is a process for the preparation of the intermediate ethyl 2-(2,6-dichlorophenoxy)propionate (III) from 2,6-dichlorophenol and ethyl 2-chloropropionate in the presence of a polar aprotic solvent and an alkali or alkaline earth carbonate salt, preferably potassium carbonate. Both processes are more cost-effective and more easily industrially scalable than the known procedures, thus enabling the active ingredient to be obtained with high yields at a limited cost.
priorityDate 2019-06-21-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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