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Synthesis of the racemate and individual enantiomers of [11C]methylphenidate for studying presynaptic dopaminergic neuron with positron emission tomography

✍ Scribed by Y.-S. Ding; Y. Sugano; J. S. Fowler; C. Salata

Publisher
John Wiley and Sons
Year
1994
Tongue
French
Weight
501 KB
Volume
34
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

Carbon‐11 labeled dl‐threo‐methylphenidate (methyl‐2‐phenyl‐2‐(2‐piperidyl)acetate, Ritalin), a psychostimulant drug widely used to treat attention deficit hyperactivity disorder, was prepared in two steps: O‐methylation of the N‐protected dl‐threo‐ritalinic acid derivative with [^11^C]methyl iodide followed by deprotection. The same strategy was applied for the preparation of C‐11 labeled individual enantiomers of threo‐methylphenidate from N‐protected d‐threo‐ or l‐threo‐ritalinic acid. The subsequent C 18 sep‐pak and reverse‐phase HPLC purification resulted in ca. 40% radiochemical yield with a total synthesis time of 40 minutes and an average specific activity of 1.5 Ci/μmole (at EOB).

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