Synthesis of 4-Maleimidobutyric Acid and Related Maleimides

Abstract

Maleimidoalkanoic acids and their activated derivatives, such as their N-hydroxysuccinimide esters, are important, though expensive, linkers for the conjugation of biomolecules. During our synthesis of UCS1025A, we have developed a chromatography-free preparation of 4-maleimidobutyric acid on a one-mole scale.

Key words

imides - condensations - maleic anhydride - aminobutanoic acid - cross-linking reagents

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CCDC 651593 contains the supplementary crystallographic data for this paper. These data can be obtained free of charge at www.ccdc.cam.ac.uk/conts/retrieving.html [or from the Cambridge Crystallographic Data Centre, 12 Union Road, Cambridge CB2 1EZ, UK, fax: [phone], E-mail: [e-mail].