Literature DB >> 20835363

Improved Syntheses of Precursors for PET Radioligands [F]XTRA and [F]AZAN.

Yongjun Gao1, Haofan Wang, Ronnie C Mease, Martin G Pomper, Andrew G Horti.   

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 [(18)F]XTRA (1) and [(18)F]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.

Entities:  

Year:  2010        PMID： 20835363      PMCID： PMC2936105          DOI： 10.1016/j.tetlet.2010.08.001

Source DB:  PubMed          Journal:  Tetrahedron Lett        ISSN： 0040-4039            Impact factor:   2.415


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Review 6.  Human brain nicotinic receptors, their distribution and participation in neuropsychiatric disorders.

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8.  Discovery of (-)-7-methyl-2-exo-[3'-(6-[18F]fluoropyridin-2-yl)-5'-pyridinyl]-7-azabicyclo[2.2.1]heptane, a radiolabeled antagonist for cerebral nicotinic acetylcholine receptor (alpha4beta2-nAChR) with optimal positron emission tomography imaging properties.

Authors:  Yongjun Gao; Hiroto Kuwabara; Charles E Spivak; Yingxian Xiao; Kenneth Kellar; Hayden T Ravert; Anil Kumar; Mohab Alexander; John Hilton; Dean F Wong; Robert F Dannals; Andrew G Horti
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Review 10.  Development of radioligands with optimized imaging properties for quantification of nicotinic acetylcholine receptors by positron emission tomography.

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Review 1.  Selected PET Radioligands for Ion Channel Linked Neuroreceptor Imaging: Focus on GABA, NMDA and nACh Receptors.

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