Arsenic complexes for potential diagnostic applications
The present invention provides radioactive arsenic complexes useful in diagnostic and therapeutic applications and methods for forming those arsenic complexes.
1. A method of producing radiolabeled phenylarsonic acid, the method comprising:
(a) contacting a radiolabeled no-carrier added arsenic acid with a monothiol to form a first solution; and
(b) contacting the first solution with a copper-based catalyst and a phenyldiazonium salt to give a second solution comprising the radiolabeled phenylarsonic acid.
2. The method of claim 1 , wherein the radiolabeled no-carrier added arsenic acid is chosen from H 3 AsO 4 or AsO 4 3− .
3. The method of claim 1 , wherein the arsenic is 77 As or 72 As.
4. The method of claim 1 , wherein the monothiol is ammonium thioglycolate.
5. The method of claim 1 , wherein the mole:mole ratio of the no-carrier added arsenic acid to monothiol ranges from about 1:10 5 to about 1:10 7 .
6. The method of claim 1 , wherein the first solution is heated to about 50° C. to about 70° C.
7. The method of claim 1 , wherein step (a) is allowed to proceed for a period of time ranging from about 30 minutes to about 1 hour.
8. The method of claim 1 , wherein the phenyldiazonium salt is tetrafluoroborate salt.
9. The method of claim 1 , wherein the phenyldiazonium salt is ethoxybenzendiazonium salt.
10. The method of claim 1 , wherein the mole:mole ratio of the reaction intermediate from step (a) to phenyldiazonium salt ranges from about 1:10 7 to about 1:10 10 .
11. The method of claim 1 , wherein the copper-based catalyst is copper(0) nanoparticles.
12. The method of claim 1 , wherein the copper-based catalyst is copper(0) nanoparticles; and the mole to mole ratio of the reaction intermediate from step (a) to copper(0) nanoparticles ranges from about 1:10 5 to about 1:10 6 .
13. The method of claim 1 , wherein step (b) is conducted at about 20° C. to about 30° C.
14. The method of claim 1 , wherein step (b) is allowed to proceed for a period of time ranging from about 30 minutes to about 1 hour.
15. The method of claim 1 , wherein the radiolabeled phenylarsonic acid is further reacted with a monothiol and a monothiol or dithiol.
16. The method of claim 15 , wherein the monothiol is ammonium thioglycolate.
17. The method of claim 15 , wherein the mole:mole ratio of the radiolabeled phenylarsonic acid to the monothiol ranges from about 1:10 5 to about 1:10 7 .
18. The method of claim 15 , wherein the dithiol is ethane-1,2-dithiol.
19. The method of claim 15 , wherein the mole:mole ratio of the radiolabeled phenylarsonic acid to the dithiol ranges from about 1:10 6 to about 1:10 8 .
20. The method of claim 1 , wherein the radiolabeled phenylarsonic acid is 2-(4-(methoxymethyl)phenyl)-1,3,2-dithiarsolane.