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. 2014 Dec 31;20(1):470–486. doi: 10.3390/molecules20010470

Table 1.

HBC of 1-[18F]fluoro-4-iodobenzene ([18F]4) and piperazine. Total RCY is related to coupling yields based on [18F]4.

graphic file with name molecules-20-00470-i001.jpg
Entry Catalyst System Base Solvent Radiochemical Conversion Yield/Reaction Time
1 Pd2(dba)3/DavePhos NaO tBu Toluene 70%/15 min
2 Pd2(dba)3/RuPhos NaO tBu Toluene 73%/15 min
3 [CinnamylPdCl]2/BrettPhos NaO tBu Toluene 25%/30 min
4 Pd(OAc)2/RuPhos NaO tBu Toluene 60%/5 min 74%/10 min
5 Pd2(dba)3/DavePhos NaO tBu 1,4-dioxane 40%/30 min
6 Pd2(dba)3/DavePhos NaO tBu DMF 0%/60 min
7 Pd(OAc)2/RuPhos NaO tBu DMF 0%/60 min
8 [P(tBu)3PdBr]2 K3PO4 DMF 0%/60 min
9 [P(tBu)3PdBr]2 K2CO3 DMF 0%/60 min
10 Pd2(dba)3/RuPhos K3PO4 DMF 50%/6 min 88%/15 min
11 Pd[P(tBu)3]2 K3PO4 DMF 31%/15 min
12 Pd2(dba)3/JohnPhos K3PO4 DMF 67%/15 min
13 Pd2(dba)3/JohnPhos Cs2CO3 DMF 51%/15 min
14 Pd2(dba)3/XPhos K3PO4 DMF 28%/15 min
15 Pd2(dba)3/XPhos Cs2CO3 DMF 11%/15 min
16 Pd2(dba)3/RuPhos K3PO4 DMSO 60%/15 min
17 Pd2(dba)3/RuPhos Cs2CO3 DMSO ~95%/15 min
18 Pd2(dba)3/JohnPhos K3PO4 DMSO 82%/15 min
19 Pd2(dba)3/XPhos K3PO4 DMSO 77%/15 min