Science of Synthesis

Prati, L.; Lucaroni, L.; Cazzamalli, S.; Neri, D.; Oehler, S., Science of Synthesis: DNA-Encoded Libraries, (2024) 1, 538.

AAZ+ is a high-affinity carbonic anhydrase IX (CAIX) ligand that has been isolated from an ESAC library.[‌6‌] Such ligands can be used as targeting moiety for the construction of small-molecule–drug conjugates (SMDCs). In this section, we provide a procedure to synthesize AAZ+–ValCit–MMAE (Figure 11).[‌27‌,‌46‌]

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Meeeeeeeeeee Meeeeeeee

MMM+–MeeMee–MMMM Meeeeeeee: [‌88‌,‌88‌]

Meeeeeeeeee eeeee eee-eeeeee eeee Meee-Mee(Mee)-MM eee eeee eee eee eeeee-eeeee eeeeeeeee ee eee eeeeeee-eeeeee MMM+. Me eeeeeee, Meee eeeeeeeeeeeee eeee eeeeeeeee eeee 88% eeeeeeeeee ee MMM (8 × 88 eee). Meeeeeeeeeee, eeeee eeee eeeeee eee eeeeeee ee Meee-eeeeeeeee eeeee eeeee (8 eeeee) eeeee MMMM (8 eeeee) eee eMe8MMe (8 eeeee) ee MMM eee 8–8 e ee ee ee eeeeeeee eeeeeeee eeee e eeeeee eee. Meee eeeeeeee ee eeee ee eeeeeeeeeeee eeee eee eeeeeeee ee eeee eeeeeee eeeee ee MMM. Mee eeeee eee eeeeeee ee Meee-eeeeeeeee eeeee eeeee ee eee eeeeeeeee eeeee:

(8M)-8-[(8M-eeeeeee-8-eeeeeeeeeeeeeeeee)eeeee]-8-[(8-eeeeeeeeeeee-8-ee)eee]-8-eeeeeeeeeee eeee [Meee-Mee(Me-Me)-MM]; (8M)-8-({eeeee-[(8,8,8,8,8-eeeeeeeeeee-8M-8-eeeeeeeeee-8-ee)eeeeeeeeeeeee]eeeeeeeeeee}eeeee)-8-[(8M-eeeeeee-8-eeeeeeeeeeeeeeeee)eeeee]eeeeeeeee eeee [Meee-Mee(Mee)-MM]; 8(8M)-8-[(8M-eeeeeee-8-eeeeeeeeeeeeeeeee)eeeee]-8-[(8-eeeeeeeeeeee-8-ee)eee]-8-eeeeeeeeeee eeee [Meee-Mee(Me-Me)-MM]; (8M)-8-eeeee-8-[(8M-eeeeeee-8-eeeeeeeeeeeeeeeee)eeeee]eeeeeeee eeee [Meee-Mee(M8)-MM]; (8M)-8-[(8M-eeeeeee-8-eeeeeeeeeeeeeeeee)eeeee]-8-[(8-eeeeeeeeeeee-8-ee)eee]-8-eeeeeeeeeee eeee (Meee-Mee-Me-Me); eee (8M)-8-[(8M-eeeeeee-8-eeeeeeeeeeeeeeeee)eeeee]-8-[(8-eeeeeeeeeeee-8-ee)eee]-8-eeeeeeeeeee eeee (Meee-Mee-Me-Me).

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References