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Synthesis 2014; 46(10): 1399-1406
DOI: 10.1055/s-0033-1340980
DOI: 10.1055/s-0033-1340980
paper
Scalable and Cost-Effective Synthesis of a Linker for Bioconjugation with a Peptide and a Monoclonal Antibody
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Further Information
Publication History
Received: 24 January 2014
Accepted after revision: 20 February 2014
Publication Date:
17 March 2014 (online)
Abstract
An efficient, scalable, and cost-effective synthesis of a linker employed in a bioconjugation process with a peptide and a monoclonal antibody is presented. Several routes were investigated that resulted in the identification of a short synthesis to a key acid intermediate from inexpensive and readily available starting materials. The final coupling of this acid with an aniline to afford the desired linker has been optimized to produce multi-gram quantities of material for clinical studies. The very limited purifications needed for both intermediates and final product make this route amenable to scale.
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