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Synthesis of boronated acridine carboxylic acid as a possible agent for BNCT.
Uppsala University, Teknisk-naturvetenskapliga vetenskapsområdet, Chemistry, Department of Chemistry.
Manuscript (Other academic)
URN: urn:nbn:se:uu:diva-90779OAI: oai:DiVA.org:uu-90779DiVA: diva2:163252
Available from: 2003-09-09 Created: 2003-09-09 Last updated: 2010-01-13Bibliographically approved
In thesis
1. Carborane Derivatives for Nuclide Therapy and Imaging: Synthesis and Radio-labelling
Open this publication in new window or tab >>Carborane Derivatives for Nuclide Therapy and Imaging: Synthesis and Radio-labelling
2003 (English)Doctoral thesis, comprehensive summary (Other academic)
Abstract [en]

This thesis describes synthesis and radiohalogenation of closo-carborane and nido-carborate derivatives for application in nuclide therapy and imaging. The work could be divided in to four sections.

In the first section, the synthesis of three boronated DNA-intercalators – 1–(N-9-acridinyl-3-aminopropyl)-para-carborane-12-carboxylic acid hydrogen chloride, 1-[1-(N-9-acridinyl-3-aminopropyl)-para-carborane 12-(3-propyloxi)]-1,3-propanediol, 1-(N-9-acridinyl-3-amino-propyl)-1-ortho-carborane-2-ylmethoxy)1-3-propandiol – for potential use in BNCT, using targeted delivery is described.

The second section describes the application of the Heck-reaction to 2-iodo-para-carborane, which has successfully been reacted with a number of styrene derivatives, i.e. para-phenyl, chloro, bromo, nitro, methoxy, and methyl-styrene, to furnish the desired trans-β-2-B-para-carborane)styrene.

In the third section, radio-iodination and radio-bromination of closo-carboranes is described. Reaction of the corresponding iodinated carborane, in the presence of palladium catalyst, [125I]iodinated and [76Br]brominated carboranes were obtained in high to excellent yields.

Section four describes a method for indirect radiolabelling of antibodies with 76Br. It was shown that NBI, a isothiocyanatobenzene derivative of dodecahydro-7,8-dicarba-nido-undecaborate anion, could be radio-brominated using oxidative conditions. The radio-brominated NBI was thereafter conjugated to anti-HER2 antibody for biological evaluation.

Place, publisher, year, edition, pages
Uppsala: Acta Universitatis Upsaliensis, 2003. 52 p.
Comprehensive Summaries of Uppsala Dissertations from the Faculty of Science and Technology, ISSN 1104-232X ; 881
Organic chemistry, Organisk kemi
National Category
Organic Chemistry
Research subject
Organic Chemistry
urn:nbn:se:uu:diva-3561 (URN)91-554-5722-3 (ISBN)
Public defence
2003-10-02, B22, BMC, Uppsala, 10:15 (English)
Available from: 2003-09-09 Created: 2003-09-09 Last updated: 2009-11-23Bibliographically approved

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