The synthesis of 14C-labeled N-succinimidyl-3-maleimidopropionate, a linker molecule for PEGylated biologics

Carbon‐14 labeled linker molecule, N‐succinimidyl‐3‐maleimidopropionate was prepared for disposition studies of PEGylated biologics. Our new route started with 100 mCi of carbon‐14 labeled Potassium cyanide (KCN) to prepare 55 mCi of [1‐14C]N‐succinimidyl‐3‐maleimidopropionate, 6 in five steps. This...

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Bibliographic Details
Published in:Journal of labelled compounds & radiopharmaceuticals 2014-10, Vol.57 (12), p.667-669
Main Authors: Cao, Kai, Maxwell, Brad D., Bonacorsi, Samuel J.
Format: Article
Language:eng ; fre ; ger
Subjects:
Carbon Radioisotopes - chemistry
carbon-14
linker molecule
Maleimides - chemical synthesis
Maleimides - chemistry
N-succinimidyl-3-maleimidopropionate (BMPS)
PEGylated biologics
Polyethylene Glycols - chemistry
Radiopharmaceuticals - chemical synthesis
Radiopharmaceuticals - chemistry
Succinimides - chemical synthesis
Succinimides - chemistry
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Summary:Carbon‐14 labeled linker molecule, N‐succinimidyl‐3‐maleimidopropionate was prepared for disposition studies of PEGylated biologics. Our new route started with 100 mCi of carbon‐14 labeled Potassium cyanide (KCN) to prepare 55 mCi of [1‐14C]N‐succinimidyl‐3‐maleimidopropionate, 6 in five steps. This represents a multiple of 5.5× improvement in the yield of the desired labeled product compared with our previous synthesis. From carbon 14 labeled potassium cyanide, the linker molecule [1‐14C]N‐succinimidyl‐3‐maleimidopropionate was prepared in five steps in 55% radiochemical yield. This is a 5.5 times improvement in yield compared with our earlier synthesis.
ISSN:0362-4803
1099-1344
DOI:10.1002/jlcr.3225