Improved synthesis and radiolabeling of [11C]MP4A, a suitable ligand for the investigation of the cholinergic system using PET.
An improved synthesis of the precursor acetic acid-piperidine-4-yl ester by acetylation of 4-hydroxypiperidine hydrochloride in anhydrous chloroform was developed. A procedure for fast evaluation and characterization of products originated by acetylation of the 4-piperidinol using LC-APCI/MS with an acetonitrile-water gradient method on a Merck Purosphere RP-18 column was also developed. The highly purified precursor allowed the production of [11C]MP4A for PET studies of acetylcholine neurotransmission system. The tracer was produced with >98% radiochemical purity, with yields ranging 20-60% (decay-corrected) from EOB.
Carpinelli
A
A
IBFM-CNR, Scientific Institute, University of Milano Bicocca, H. S. Raffaele, Via Olgettina 60, 20132 Milano, Italy. carpinelli.assunta@hsr.it
Magni
F
F
Cattaneo
A
A
Matarrese
M
M
Turolla
E
E
Todde
S
S
Bosso
N
N
Galli Kienle
M
M
Fazio
F
F
D000085:Acetates / Q000138:chemical synthesis* / Q000737:chemistry; D000107:Acetylation; D000110:Acetylcholinesterase / Q000032:analysis; D002851:Chromatography, High Pressure Liquid; D008401:Gas Chromatography-Mass Spectrometry; D006801:Humans; D006847:Hydrocarbons, Iodinated / Q000737:chemistry*; D007553:Isotope Labeling / Q000379:methods; D009682:Magnetic Resonance Spectroscopy; D010880:Piperidines / Q000138:chemical synthesis* / Q000737:chemistry; D049268:Positron-Emission Tomography / Q000379:methods; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000737:chemistry
D000085:Acetates; D006847:Hydrocarbons, Iodinated; C100518:N-methyl-4-piperidyl acetate; D010880:Piperidines; D019275:Radiopharmaceuticals; C014055:methyl iodide; D000110:Acetylcholinesterase