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. Author manuscript; available in PMC: 2020 Mar 5.
Published in final edited form as: Chem Commun (Camb). 2019 Mar 5;55(20):2976–2979. doi: 10.1039/c9cc00641a

Table 2.

Radiofluorination Optimization Studiesa

graphic file with name nihms-1021710-t0005.jpg
Entry [Pd] Oxidant RCY (%)#
1 Pd(OAc)2 PhI(OPiv)2 3±1 (n=2)
2 Pd(OAc)2 PhI(OPiv)2 8±2b (n=2)
3 Pd(OAc)2 PhI(OAc)2 11±2b (n=2)
4 Pd(OAc)2 PhI(OAc)2 13±1b,c (n=2)
5 Pd2(dba)3 PhI(OAc)2 18±2b(n=2)
6 Pd2(dba)3 PhI(OAc)2 21±5b,d (n=7)
7 Pd2(dba)3 PhI(OAc)2 51±10 (n = 2)b,e
a

General conditions: aliquots of a prestirred stock solution containing Ag[18F]F (92.5–129.5 MBq) and oxidant (2 equiv) in CH2Cl2 (200 μL) were added to vials containing substrate (0.014 mmol) and [Pd] (10 mol %) in CH2Cl2 (550 μL);

b

reaction included pre-stirring step;

c

C2H4Br2:CH2Cl2 [2:1] used as reaction solvent;

d

3-fold scale up of substrate (0.042 mmol) while retaining stoichiometry of other reactants/reagents;

e

5 equiv. AgF added to reaction.