[11 C] Olanzapine, radiosynthesis and lipophilicity of a new potential PET 5-HT 2 and D 2 receptor radioligand

M Gao, Z Shi, M Wang, QH Zheng

Index: Gao, Mingzhang; Shi, Zenas; Wang, Min; Zheng, Qi-Huang Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 7 p. 1953 - 1956

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Citation Number: 12

Abstract

Olanzapine and its precursor desmethyl-Olanzapine were synthesized from malononitrile, propionaldehyde, 1-fluoro-2-nitrobenzene, and substituted piperazine in 4, 4, 5, and 5 steps with 35%, 32%, 26%, and 32% overall chemical yield, respectively.[11C] Olanzapine was prepared from desmethyl-Olanzapine with [11C] CH3OTf through N-[11C] methylation and isolated by HPLC combined with solid-phase extraction (SPE) in 40–50% radiochemical ...