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. 2020 Oct 9;59(50):22494–22499. doi: 10.1002/anie.202006725

Scheme 1.

Scheme 1

Solid‐phase supported strategy for the parallel synthesis of DNA‐alkylating HDACi hybrid molecules. a.) PhthN‐OH (3.5 equiv), Et3N (3.5 equiv), DMF, r.t., 48 h. b.) 5 % N2H4⋅H2O in MeOH, r.t., 2× 15 min. c.) Fmoc‐NH‐Linker‐COOH (2.0 equiv), HATU (2.0 equiv), HOBt⋅H2O (2.0 equiv), DIPEA (3.0 equiv), DMF, r.t., 20 h. d.) 20 % piperidine in DMF, 2x 5 min. e.) Cap‐COOH (3.0 equiv), HATU (3.0 equiv), DIPEA (5.0 equiv), DMF, r.t., 20 h, dark environment. f.) 5 % TFA in CH2Cl2, r.t.,1 h.