http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-3468620-A2

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filingDate 2017-03-07-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c9531201c66ace4f80006630bac9d5f4
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publicationDate 2019-04-17-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber EP-3468620-A2
titleOfInvention 18 f-labeled bisphosphonates for pet imaging
abstract A novel method for rapidly and efficiently introducing fluorine into the P-C-P backbone of bisphosphonates starting from readily accessible diazomethylenebisphosphonate esters is provided. The method is applied successfully to create novel [ 18 F]-labeled bisphosphonates for positron emission tomography imaging. Some versions of the method include reacting a diazomethylenebisphosphonate tetraalkyl ester with a fluorinating agent in the presence of an acidic HF/base complex and a t -butyl hypohalite to produce a halofluoromethylenebisphosphonate tetraalkyl ester, and dealkylating the halofluoromethylenebisphosphonate alkyl ester to produce a halofluoromethylenebis(phosphonic acid). Methods of replacing the halogen group with hydrogen are further provided. 18 F-labeled bisphosphonates prepared by the methods, and methods of using such compounds for positron emission tomography imaging in patients and animal models, are also provided.
priorityDate 2016-03-07-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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