Dithiol Aryl Arsenic Compounds as Potential Diagnostic and Therapeutic Radiopharmaceuticals.
Journal Article (Journal Article)
Arsenic-72 ((72)As) and (77)As have nuclear properties useful for positron emission tomography (PET) and radiotherapy, respectively. The thiophilic nature of arsenic led to the evaluation of dithioarylarsines for potential use in radiopharmaceuticals. Several dithioarylarsines were synthesized from their arylarsonic acids and dithiols and were fully characterized by NMR, ESI-MS, and X-ray crystallography. This chemistry was translated to the no-carrier-added (nca) (77)As level. Because arsenic was available at the nca nanomolar level only as [(77)As]arsenate, this required addition of an aryl group directly to the As to form the [(77)As]arylarsonic acid. The [(77)As]arsenate was reduced from (77)As (V) to (77)As (III), and a modified Bart reaction was used to incorporate the aryl ring onto the (77)As, which was followed by dithiol addition. Various modifications and optimizations resulted in 95% radiochemical yield of nca [(77)As]p-ethoxyphenyl-1,2-ethanedithiolatoarsine.
Full Text
Duke Authors
Cited Authors
- DeGraffenreid, AJ; Feng, Y; Wycoff, DE; Morrow, R; Phipps, MD; Cutler, CS; Ketring, AR; Barnes, CL; Jurisson, SS
Published Date
- August 15, 2016
Published In
Volume / Issue
- 55 / 16
Start / End Page
- 8091 - 8098
PubMed ID
- 27453472
Electronic International Standard Serial Number (EISSN)
- 1520-510X
Digital Object Identifier (DOI)
- 10.1021/acs.inorgchem.6b01175
Language
- eng
Conference Location
- United States