Radiosynthesis and Preclinical Evaluation of ¹¹C-VA426, a Cyclooxygenase-2 Selective Ligand

Table 1

Radiosynthesis summary of ¹¹C-VA426.

VA425	DMSO	Base^a	Amount of base	Rad. yield^b (%)	SA^c	N^d
3.2 mg (8.6 μmol)	150 μl	tBuOK	1.5 mg (13 μmol)	15 ± 2	37–148 GBq/μmol	20
2 mg (5.4 μmol)	200 μl	NaH 60%	2 mg (50 μmol)	7 ± 2	37–111 GBq/μmol	20
2 mg (5.4 μmol)	200 μl	NaOH 1N	2 mg (2 μmol)	5 ± 2	37–74 GBq/μmol	5

^aInfluence of the base. ^bRadiochemical yield (n.d.c. from [¹¹C]MeOTf). ^cMolar activity. ^dNumber of runs. The reaction was carried out at 80°C for 2 minutes.