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Synthesis 1991; 1991(10): 819-821
DOI: 10.1055/s-1991-26579
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Facile Synthesis of Reagents Containing a Terminal Maleimido Ligand Linked to an Active Ester

Ole Nielsen* , Ole Buchardt
  • *Research Center for Medical Biotechnology, Chemical Laboratory II, The H. C. Ørsted Institute, University of Copenhagen, Universitetsparken 5, DK-2100 Copenhagen, Denmark
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Publication Date:
29 April 2002 (online)

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Condensation of ω-amino acids with maleic anhydride to yield maleamino acids and subsequent esterification with N-hydroxysuccinimide, 3,4-dihydro-3-hydroxy-4-oxo-1,2,3-benzotriazine, or pentafluorophenol to give the corresponding esters in a one pot procedure are described. The reagents can be isolated and purified without chromatography in 7-55% yields.