A new facile synthetic route to [11 C] GSK189254, a selective PET radioligand for imaging of CNS histamine H 3 receptor

…, BE Glick-Wilson, C Brown-Proctor, A Shekhar…

Index: Wang, Min; Gao, Mingzhang; Steele, Brandon L.; Glick-Wilson, Barbara E.; Brown-Proctor, Clive; Shekhar, Anantha; Hutchins, Gary D.; Zheng, Qi-Huang Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 14 p. 4713 - 4718

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Citation Number: 14

Abstract

GSK189254 and its corresponding precursor GSK185071B were synthesized from 3- methoxyphenylacetic acid with 6-chloropyridine-3-carbolic acid or 6-chloronicotinamide in 8 and 7 steps with either 6% or 7% and either 14% or 16% yield, respectively.[11C] GSK189254 was prepared from GSK185071B with [11C] CH3OTf through N-[11C] methylation and isolated by HPLC combined with solid-phase extraction (SPE) in 50–60% ...

~96%

~53%

~64%

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