Effect of tellurium position on the myocardial uptake of radioiodinated 18-iodotellura-17-octadecenoic acid analogs
作者:F. F. Knapp、P. C. Srivastava、A. P. Callahan、E. B. Cunningham、G. W. Kabalka、K. A. R. Sastry
DOI:10.1021/jm00367a011
日期:1984.1
myocardial specificity and retention of fatty acids in which radioiodide is stabilized as a trans-(E)-vinyl iodide has been evaluated in rats. Five analogues of 18-iodo-17-octadecenoic acid (ICH = CH-R-Te-R'-COOH) with Te at positions 5, 7, 9, 11, and 13 were prepared by coupling of a trans-diiodoalkene (ICH = CH-R-I) with the requisite sodium [(alkoxycarbonyl)alkyl]telluride substrate (NaTe-R'-COOR";
已经在大鼠中评估了碲位置对心肌特异性和其中放射性碘稳定为反式-(E)-乙烯基碘的脂肪酸保留的影响。通过反式二碘代烯烃(ICH)的合成,制备了5个18-碘-17-十八碳烯酸(ICH = CH-R-Te-R'-COOH)在5、7、9、11和13位带有Te的类似物。用必需的[(烷氧基羰基)烷基]碲化钠钠(NaTe-R'-COOR”; R” = Me或Et),然后进行碱性水解。通过改变R和R',制备了一系列具有18个碳原子的链长的类似物。通过NaBH4还原相应的二碲化物原位生成碲化物底物,并通过碘化钠-氯胺-T处理相应的乙烯基硼酸[(HO)2BCH = CH-RI)]制备二碘代烯烃。通过用儿茶酚硼烷处理由市售材料合成的末端乙炔(HC与CRI相同)来制备乙烯基硼酸。所有新化合物均通过TLC,NMR,MS和元素分析进行了分析。以相同方式制备125I类似物[(E)-125ICH = CH-R-Te-