title: The synthesis of 14C-labeled N-succinimidyl-3-maleimidopropionate, a linker molecule for PEGylated biologics.
abstract: 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-(14)C]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.
authors.affiliation: Department of Chemical Synthesis, Radiochemistry Group, Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research and Development, P.O. Box 4000, Princeton, NJ, 08543, USA.
authors.forename: Kai
authors.initials: K
authors.lastname: Cao
authors.forename: Brad D
authors.initials: BD
authors.lastname: Maxwell
authors.forename: Samuel J
authors.initials: SJ
authors.lastname: Bonacorsi
mesh_terms: D002250:Carbon Radioisotopes / Q000737:chemistry; D008301:Maleimides / Q000138:chemical synthesis* / Q000737:chemistry; D011092:Polyethylene Glycols / Q000737:chemistry; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000737:chemistry; D013388:Succinimides / Q000138:chemical synthesis* / Q000737:chemistry
chemical_list: D002250:Carbon Radioisotopes; D008301:Maleimides; D019275:Radiopharmaceuticals; D013388:Succinimides; C075481:succinimidyl 3-N-maleimidopropionate; D011092:Polyethylene Glycols
keywords: N-succinimidyl-3-maleimidopropionate (BMPS); PEGylated biologics; carbon-14; linker molecule