Improved syntheses of precursors for PET radioligands [18F]XTRA and [18F]AZAN

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

Research output: Contribution to journalArticlepeer-review

5 Scopus citations


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.

Original languageEnglish (US)
Pages (from-to)5333-5335
Number of pages3
JournalTetrahedron Letters
Issue number40
StatePublished - Oct 6 2010


  • N-Methylation
  • PET radioligand
  • Stille coupling
  • nAChR

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry


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