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Updated: Aug 29, 2025

Synthesis and Bioconjugation of Thiol-Reactive Reagents for the Creation of Site-Selectively Modified Immunoconjugates
Published on: March 6, 2019
A two-site reactive platform in the synthesis of amino-functionalized amphiphilic molecules via sulfenic acids
Paola Bonaccorsi1, Chiara Maria Antonietta Gangemi1, Valentina Greco2
1Dipartimento di Scienze Chimiche Biologiche Farmaceutiche ed Ambientali (CHIBIOFARAM), Università degli Studi di Messina, Sicily, Italy. abarattucci@unime.it.
Abstract:
The synthesis of some bolaamphiphiles is described. It is a convergent approach that allows the linkage of a glucosyl derivative to a bis-functionalized platform, via a copper-free Sonogashira cross-coupling. The central core was obtained from the reaction of a suitably substituted bis-sulfoxide with diethynyl benzenes. The intermediates of such reaction are sulfenyl functions that are easily added to one triple bond of the unsaturated molecules. The functionalization at the central core, through the nucleophilic addition of ammonia or piperidine onto the two vinyl sulfonyl groups already present in the backbones of the molecules, opened the way to the preparation of more complex derivatives. The observation of the formation of new stereogenic carbons with an unexpected significantly high diastereoselectivity was justified and supported by preliminary theoretical calculations. The two ending glucosyl moieties were favourably deprotected to afford the amino-functionalized bolaamphiphilic molecules.
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