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. 2016 Aug 30;7(11):994–998. doi: 10.1021/acsmedchemlett.6b00253

Scheme 1. Overview of the Tandem-Knoevenagel Condensation–Michael Addition Ligation Using a Pyrazolone Nucleophile.

Scheme 1

(A) Generation of a DAR 4 site-specific ADC via first addition of pyrazolone via Knoevenagel condensation, then subsequent second addition of pyrazolone via Michael addition. (B) Previously published trapped-Knoevenagel ligation. (C) Double addition of pyrazolone to reducing sugar via a tandem Knoevenagel condensation–Michael addition.