Synthesis procedure for routine production of [carbonyl-11C]desmethyl-WAY-100635.
An improved one-pot synthesis procedure for routine production of [carbonyl-(11)C]desmethyl-WAY-100635 ([(11)C]DWAY) is described. An efficient purification of the crude product has also been developed and was accomplished by C-18 reversed-phase semi-preparative HPLC using 55/45 EtOH-NaH(2)PO(4) buffer (20 mM, pH=6.5) as the eluent. The desired product fraction was collected in a 2.0-2.5 mL volume and formulated with 11 mL of 0.9% saline. The radioligand was ready for human use in 45 min (EOB). The product was obtained with a radiochemical yield of 11.1+/-1.8% (EOB, n=15) with a radiochemical purity of >99%. Specific activity was 133.2-185.0 GBq/micromol (3.6-5.0 Ci/micromol, EOS, n=2) when ca. 37.0 GBq (ca. 1.0 Ci) of starting [(11)C]CO(2) was used. Unlabeled mass of [(11)C]DWAY was found to be 0.15-0.24 microg/mL and the precursor was present in less than 50 ng/mL in final production solution.
Maiti
Dilip K
DK
Department of Pediatrics, School of Medicine, PET Center, Children's Hospital of Michigan, Wayne State University, Detroit, MI 48201, USA.
Chakraborty
Pulak K
PK
Chugani
Diane C
DC
Muzik
Otto
O
Mangner
Thomas J
TJ
Chugani
Harry T
HT
D002250:Carbon Radioisotopes; D002855:Chromatography, Thin Layer / Q000379:methods; D010879:Piperazines / Q000138:chemical synthesis* / Q000302:isolation & purification; D011725:Pyridines / Q000138:chemical synthesis* / Q000302:isolation & purification; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000302:isolation & purification
D002250:Carbon Radioisotopes; D010879:Piperazines; D011725:Pyridines; D019275:Radiopharmaceuticals; C112544:desmethyl-WAY 100635