Synthesis and radioiodination of a nido-1,2-carboranyl derivative of 2-nitroimidazole

ORCiD

0000-0001-9010-5970

Document Type

Article

Publication Title

Nuclear Medicine and Biology

ISSN

0969-8051

Volume

21

Issue

4

DOI

10.1016/0969-8051(94)90025-6

First Page

601

Last Page

611

Publication Date

5-1-1994

Abstract

The synthesis of a nido-carboranyl congener of misonidazole, 1-(3′-nido-carboranyl-2′-hydroxy)propyl-2-nitroimidazole, has been carried out. Alternative methods of preparations were conducted to optimize the chemical yield, with a five step synthesis giving an overall yield (from 1,2-carborane) of 36%. A diastereomeric pair of nido-carboranyl compounds was obtained. The diastereomeric nido-carboranyl misonidazole congeners were (radio)iodinated to yield (> 90%) a mixture of diastereomeric compounds in which the iodine had bonded to a boron atom on the nido-carborane moiety. These compounds will be investigated for their application to boron neutron capture therapy (BNCT) and hypoxia imaging of cancer.

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