一些巢式和闭式单碳碳硼烷衍生物的合成、放射性碘化及生物分布

Synthesis, radioiodination, and biodistribution of some nido- and closo-monocarbon carborane derivatives.

作者信息

Wilbur D Scott, Hamlin Donald K, Srivastava Rajiv R, Chyan Ming-Kuan

机构信息

Department of Radiation Oncology, University of Washington, 2121 N. 35th Street, Seattle, WA 98103, USA.

出版信息

Nucl Med Biol. 2004 May;31(4):523-30. doi: 10.1016/j.nucmedbio.2003.11.003.

DOI:10.1016/j.nucmedbio.2003.11.003

PMID:15093823

Abstract

Iodination and radioiodination reactions of several anionic nido- and closo-monocarbon carboranes were conducted. Iodinations occurred more rapidly with nido-carboranes than with closo-carboranes. The most rapid iodination and radioiodination reactions occurred with unsubstituted carboranes. C-amino and C-ammonium derivatives did not iodinate under the conditions studied. Both nido- and closo-carboranes with C-NH-acetyl and C-NH-succinyl substituents iodinated, but the nido-carboranes iodinated under milder reaction conditions. Biodistributions of nido-1-succinylamido-[(131)I]carborane and closo-1-succinylamido-[(125)I]carborane were similar in mice, but blood clearance of the nido- compound was slower.

摘要

对几种阴离子型巢式和闭式单碳碳硼烷进行了碘化和放射性碘化反应。巢式碳硼烷的碘化反应比闭式碳硼烷更快。未取代的碳硼烷发生的碘化和放射性碘化反应最快。在研究的条件下，C-氨基和C-铵衍生物不发生碘化反应。带有C-NH-乙酰基和C-NH-琥珀酰基取代基的巢式和闭式碳硼烷都能发生碘化反应，但巢式碳硼烷在较温和的反应条件下发生碘化反应。巢式-1-琥珀酰氨基-[(131)I]碳硼烷和闭式-1-琥珀酰氨基-[(125)I]碳硼烷在小鼠体内的生物分布相似，但巢式化合物的血液清除较慢。