6-[¹⁸F]Fluoro-L-DOPA: A Well-Established Neurotracer with Expanding Application Spectrum and Strongly Improved Radiosyntheses

Table 1

Selected synthesis details from electrophilic fluorination reactions for the synthesis of [¹⁸F]F-DOPA.

Radiolabeling method	Time [min]	RCY [%]^a	Impurities in product	SA [MBq/μmol]	ee [%]	Citation
Desilylation	60	8^b	n. d.	25.2	100	Diksic and Farrokhzad ’85 [42]
L-DOPA + BF3	120	18	n. d.	n. d.	100	Chirakal et al. ’86 [92]
Demercuration	65	12	<10 ppb Hg	n. d.	97	Adam and Jivan ’88 [43]
Demercuration	50	11	<20 ppb Hg	2.6	>99	Luxen et al. ’90 [44]
Destannylation	60	25	<15 ppb Sn	n. d.	>99	Namavari et al. ’92 [47]
O-Pivaloyl ester of L-DOPA	60	17 ± 1.9	n. d.	17 ± 2.5	100	Ishiwata et al. ’93 [93]
Demercuration	45–50	14^b	<0.05 μg/mL Hg	17–19	>98	Chaly et al. ’93 [94]
Destannylation	45–50	26	1.5–2.5 ppm Sn	4.4	>99	Dollé et al. ’98 [48]
Destannylation	50	25 ± 3	<1 μg/mL CDCl3	30 ± 2	96 ± 1	Füchtner et al. ’08 [95]

aUnless otherwise stated, RCYs are given decay corrected (d. c.) and ^bnondecay corrected (n. d. c.).