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. Author manuscript; available in PMC: 2019 May 15.
Published in final edited form as: J Labelled Comp Radiopharm. 2018 Apr 17;61(5):427–437. doi: 10.1002/jlcr.3606

Table 2.

Optimization of MDL100907 synthesis using tracer-level [19F]KFa

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Entry Precursor (mg) K2CO3 (mg) K222 (mg) Catalystb Solvent (mL) T (˚C) % conv.
R = H 1 5 2.8 14 Cu(OTf)2(py)4 DMF 0.3 110 n/a
2 5 2.8 14 Cu(OTf)2 DMF 0.3 110 n/a
3 5 0.060 0.28 Cu(OTf)2 DMF 0.3 110 n/a
4 5 0.060 0.28 Cu(OTf)2(py)4 DMF 0.3 110 n/a
R = Bocc 5 5 2.8 14 Cu(OTf)2(py)4 DMF 0.3 110 n/a
6 5 0.060 0.28 Cu(OTf)2(py)4 DMF 0.3 110 18.1
7 10 0.060 0.28 Cu(OTf)2(py)4 DMF 0.3 110 17.0
8 5 0.060 0.28 Cu(OTf)2(py)4 DMF 0.3 120 16.9
9 5 0.060 0.28 Cu(OTf)2(py)4 DMF 0.3 100 15.5
10 5 0.060 0.28 Cu(OTf)2(py)4 DMF 0.2 110 14.8
11 5 0.060 0.28 Cu(OTf)2(py)4d DMF 0.3 110 11.3
12 2.5 0.060 0.28 Cu(OTf)2(py)4 DMF 0.2 110 8.3
13 5 0.060 0.28 Cu(OTf)2 DMF 0.3 110 n/a
14 5 0.060 0.28 Cu(OTf)2(py)4 DMF:ACN 1:1 110 n/a
a

In all experiments, 0.15 μg of KF was used as the fluorine source.

b

Catalyst: precursor = 1:3 (molar ratio)

c

Deprotection of Boc group was carried out with TFA.

d

Catalyst: precursor = 1: 2