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. 2022 Jun 20;13(7):1182–1190. doi: 10.1021/acsmedchemlett.2c00124

Scheme 2. (A) NHS Esters Used in D2B Synthesis, (B) Optimization of JQ1 Amide Formation via HTE Base and Additive Screening Using Four Representative Mono-N-Boc Diamines, and (C) Three-Step D2B PROTAC Synthesis.

Scheme 2

Final conditions shown as green bars.

Bar graphs represent purity of unchromatographed PROTACs and demonstrate purity enrichment though scavenging resin treatment. Blue: desired PROTAC; yellow, orange, red: reaction byproducts.