Synthesis 2023; 55(14): 2177-2185
DOI: 10.1055/s-0042-1751436
paper

A Simple and Modular Access to 4-Mercapto-4-methylpentanoic Acid: A Useful Building Block in Antibody-Drug Conjugates Research

Logan Salamone
a   Minakem High Potent, rue Fond Jean Pâques 8, 1435 Mont-Saint-Guibert, Belgium
,
Martin Lepeintre
a   Minakem High Potent, rue Fond Jean Pâques 8, 1435 Mont-Saint-Guibert, Belgium
,
Vincent L. Revil-Baudard
a   Minakem High Potent, rue Fond Jean Pâques 8, 1435 Mont-Saint-Guibert, Belgium
,
Fabien Serpier
a   Minakem High Potent, rue Fond Jean Pâques 8, 1435 Mont-Saint-Guibert, Belgium
,
Laurent Petit
b   Minakem Recherche, 145 Chemin des Lilas, 59310 Beuvry-La-Forêt, France
› Institutsangaben


Abstract

An efficient synthesis of 4-mercapto-4-methylpentanoic acid, a fragment notably found in Antibody-Drug Conjugates (ADCs), is reported using an intermolecular radical transfer reaction as the pivotal step. The reported approach displays several advantages over more traditional routes and is compatible with the chemistry involved in the construction of ADCs. Original analogues of the molecule of interest can be readily accessed using the method developed.

Supporting Information



Publikationsverlauf

Eingereicht: 04. Januar 2023

Angenommen nach Revision: 17. Februar 2023

Artikel online veröffentlicht:
04. April 2023

© 2023. Thieme. All rights reserved

Georg Thieme Verlag KG
Rüdigerstraße 14, 70469 Stuttgart, Germany

 
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