Details

Autor(en) / Beteiligte

• Kumar, Piyush
• Wiebe, Leonard I
• Atrazheva, Elena
• Tandon, Manju

Titel

An improved synthesis of α-AZA, α-AZP and α-AZG, the precursors to clinical markers of tissue hypoxia

Ist Teil von

• Tetrahedron letters, 2001-03, Vol.42 (11), p.2077-2078

Ort / Verlag

Elsevier Ltd

Erscheinungsjahr

2001

Link zum Volltext

Quelle

Elsevier Journal Backfiles on ScienceDirect (DFG Nationallizenzen)

Beschreibungen/Notizen

• α-[ 123I]-IAZA and α-[ 123I]-IAZP are experimental diagnostic radiopharmaceuticals which have been used clinically to diagnose hypoxia in a number of pathologies, including cancer, peripheral vascular disease, rheumatoid arthritis and brain trauma. These nitroimidazole nucleosides are synthesized from the non-iodinated nucleosides AZA, AZP and AZG, respectively. Earlier methods report low chemical yields for the synthesis of these precursors. The modified procedures now reported provide nearly quantitative yields of these compounds, thereby substantially reducing the cost and effort of synthesis. An improved procedure to synthesize AZA, AZP and AZG, the precursors to clinically useful markers of a variety of hypoxia disorders, including solid tumors and cancer, is described.