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


  • eng

Conference Location

  • United States