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On-resin macrocyclization of an RGDS peptide. The following procedure was used to functionalize and macrocyclize the peptide: (a) (4 eq) 2-chloroethanesulfonyl chloride, (8 eq) TEA, r.t., for 2 h, 2 times, (b) 3% TFA/5% TES in DCM, r.t., 30 s, 15 times, and (c) 10 mol% DBU in DMF, r.t., 1 h.
