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filingDate 2000-04-10-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2001-09-11-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_bb07a3eac2ac61a38a6b41c73f999b15
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_eb432a102b494181ffd6d10e83a7da6c
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publicationDate 2001-09-11-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber US-6288224-B1
titleOfInvention Preparation of n-arylmethyl aziridine derivatives, 1,4,7,10-tetraazacyclododecane derivatives obtained therefrom and n-arylethyl-ethanolamine sulphonate esters as intermediates
abstract Aziridines may be subjeted to a cyclooligomerization reaction to produce polyazacycloalkane compounds useful for example in the preparation of chelating agents for use in diagnostic imaging contrast agents. N-benzyl-aziridine in particular is useful as it can be cyclotetramerized and debenzylated to yield cyclen, a key intermediate in chelating agent preparation. The invention provides a particularly attractive route to production of N-benzyl and other N-arylmethyl aziridines of formula (I)where each R1 is independently hydrogen or a group AR and Ar is an optionally substituted phenyl group. The process comprises reacting a purified N-arylmethylethanolamine-sulphonate sulphonate ester with a base. N-aryimethyl-ethanolamine sulphonate ester of the formula R'NHCH2CH2OSO3H, wherein the N-arylmethyl group R' is an N-(bisarylmethyl) or N-(triarylmethyl) group, as intermediates. In a further aspect, the invention provides compounds of formula (II)where Ar and R1 are as hereinabove defined and at least two differing ArCHR21 moieties are present.
priorityDate 1995-03-10-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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