Improved syntheses of precursors for PET radioligands [F]XTRA and [F]AZAN |
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| Authors: | Yongjun Gao Haofan Wang Ronnie C. Mease Martin G. Pomper Andrew G. Horti |
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| Affiliation: | Russell H. Morgan Department of Radiology and Radiological Sciences, School of Medicine, Johns Hopkins University, 600 North Wolfe Street, Baltimore, MD 21287-0816, United States |
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| Abstract: | Improved syntheses of 7-methyl-2-exo-[3′-(2-bromopyridin-3-yl)-5′-pyridinyl]-7-azabicyclo[2.2.1]heptanes (3) and 7-methyl-2-exo-[3’-(6-bromopyridin-2-yl)-5′-pyridinyl]-7-azabicyclo[2.2.1]heptanes (4), precursors for PET radioligands [18F]XTRA (1) and [18F]AZAN (2), involving a key Stille coupling step followed by deprotection of Boc group and N-methylation are described. The new synthetic procedures provided the title compounds in more than 40% overall yields. |
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| Keywords: | nAChR PET radioligand Stille coupling N-Methylation |
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