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Synthesis of 2‐14C‐iminothiolane and 2‐13C,15N‐iminothiolane (Traut's reagent)
Authors:Michael Wallace  Alban J. Allentoff  John Brailsford  Sharon Gong  Samuel Bonacorsi Jr.  Frank Rinaldi
Affiliation:1. Discovery Chemistry Platforms‐Radiochemistry, Bristol‐Myers Squibb, Princeton, NJ, USA;2. Pharmaceutical Research and Development, Bristol‐Myers Squibb, New Brunswick, NJ, USA
Abstract:2‐Iminothiolane has found utility in the growing area of antibody–drug conjugates by serving as a lysine‐thiolating agent and the junction between the antibody and the cytotoxic payload during random conjugation of a monoclonal antibody. 2‐14C‐Iminothiolane was prepared from commercially available [14C]KCN using a four‐step sequence in an overall 10% radiochemical yield. Stable‐labeled 2‐13C,15N‐iminothiolane was also prepared from [13C15N]KCN in a similar manner. The. labeled Traut's reagent produced by this sequence showed comparable reactivity as the commercially available unlabeled reagent with a representative monoclonal antibody and could serve as highly informative analytical tools to investigate antibody–drug conjugate formation via the random conjugation process.
Keywords:methyl 4‐mercaptobutyrimidate  Traut's reagent  2‐iminothiolane  monoclonal antibodies
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