Automated synthesis of 11C-acetoacetic acid, a key alternate brain fuel to glucose.
An automated, one-pot radio-synthesis module for the routine preparation of 1-[(11)C]acetoacetic acid has been developed. The enolate anion of acetone was reacted with [(11)C]CO(2) in tetrahydrofuran (THF), followed by hydrolysis and purification by ion-exchange chromatography. The total synthesis time was 18 min and radiochemical yield was 34% after decay correction. HPLC analysis showed < or =3% impurities while residual THF (< or =200 ppm) and ethanol (< or =500 ppm) were well under the tolerable limits for human studies.
Tremblay
Sébastien
S
Research Center on Aging, Sherbrooke University Geriatric Institute, 1036 Belvedere Street South, Sherbrooke, Québec, Canada J1H 4C4. Sebastien.Tremblay@USherbrooke.ca
Ouellet
René
R
Rodrigue
Serge
S
Langlois
Réjean
R
Bénard
François
F
Cunnane
Stephen C
SC
D000090:Acetoacetates / Q000032:analysis / Q000138:chemical synthesis* / Q000302:isolation & purification* / Q000378:metabolism; D000818:Animals; D001921:Brain / Q000378:metabolism; D002250:Carbon Radioisotopes / Q000032:analysis / Q000737:chemistry* / Q000302:isolation & purification* / Q000378:metabolism; D002852:Chromatography, Ion Exchange / Q000295:instrumentation / Q000379:methods*; D004340:Drug Contamination / Q000517:prevention & control; D005947:Glucose / Q000378:metabolism; D006801:Humans; D007553:Isotope Labeling / Q000295:instrumentation / Q000379:methods*; D019275:Radiopharmaceuticals / Q000032:analysis / Q000138:chemical synthesis / Q000302:isolation & purification / Q000378:metabolism; D012371:Robotics / Q000295:instrumentation / Q000379:methods*
D000090:Acetoacetates; D002250:Carbon Radioisotopes; D019275:Radiopharmaceuticals; C016635:acetoacetic acid; D005947:Glucose