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Synthesis and Bioconjugation of Thiol-Reactive Reagents for the Creation of Site-Selectively Modified Immunoconjugates
Published on: March 6, 2019
New benzotriazole-sulfonate coupling reagents and applications
Sayanta Roy1, Bhubaneswar Mandal1
1Department of Chemistry, Laboratory of Peptide and Amyloid Research, Indian Institute of Technology Guwahati Assam-781039 India bmandal@iitg.ac.in +91 361 258 2319.
None:
Amide and ester bond formation is crucial in medicinal chemistry and relies heavily on coupling reagents in both academic and industry. We report the development of new cost-effective recyclable benzotriazole-sulfonate coupling reagents in a straightforward, rapid, and easy manner. The reagents efficiently activate carboxylic acids to form amides, esters, thioesters, and peptides, with excellent yields and high chirality retention. The reagent enables drug modifications and transformations, including aldoxime-to-nitrile and carboxylic acid-to-ketone conversions. The use of green solvents effectively minimizes the environmental impact.
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