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 [C-11]MP4A for PET studies of acethylcholine neurotransmission system. The tracer was produced with > 98% radiochemical purity, with yields ranging 20-60% (decay-corrected) from EOB. (c) 2005 Elsevier Ltd. All rights reserved.
Carpinelli, A., Magni, F., Cattaneo, A., Matarrese, M., Turolla, E., Todde, S., et al. (2006). Improved synthesis and radiolabeling of [C-11]MP4A, a suitable ligand for the investigation of the cholinergic system using PET. APPLIED RADIATION AND ISOTOPES, 64(2), 182-186 [10.1016/j.apradiso.2005.07.014].
Improved synthesis and radiolabeling of [C-11]MP4A, a suitable ligand for the investigation of the cholinergic system using PET
MAGNI, FULVIO;CATTANEO, ALICE SILVIA;TUROLLA, ELIA ANNA;TODDE, SERGIO CAMILLO;KIENLE, MARZIA DONATELLA;FAZIO, FERRUCCIO
2006
Abstract
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 [C-11]MP4A for PET studies of acethylcholine neurotransmission system. The tracer was produced with > 98% radiochemical purity, with yields ranging 20-60% (decay-corrected) from EOB. (c) 2005 Elsevier Ltd. All rights reserved.
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