172607-47-5Relevant academic research and scientific papers
Synthesis and authentication of iodoazidophenpyramine, a photoaffinity reporter ligand previously used for histamine H1-receptor labelling
Sorba,Tertiuk,Ganellin
, p. 677 - 680 (2007/10/03)
The synthesis is described of aminophenpyramine (7) (N-{5-[2-(4-aminophenyl)ethanamido]pentanyl}-N'-(4-methoxybenzyl)-N- methyl-N'-(2-pyridinyl)-1,2-ethandiamine), its monoiodo- and diiodo-derivatives (8 and 9), and iodoazidophenpyramine (1). The last compound is synthesised by two different routes to confirm the identity of the [125I]iodinated ligand previously made only in solution and used for characterisation of the hitamine H1-receptor protein. The procedures employ the novel intermediates 4-amino-3-iodo-phenylacetic acid (11) and 4-azido-3-iodo-phenylacetic acid (13). They have general applicability to the synthesis of non-radioactive iodinated photoaffinity receptor ligands which may be required for chemical authentication of the corresponding radiolabelled compounds.
