Skip to main content
. Author manuscript; available in PMC: 2013 Nov 28.
Published in final edited form as: J Am Chem Soc. 2012 Nov 14;134(47):19338–19341. doi: 10.1021/ja309085b

Figure 1. Synthesis of PEG-Fluorochrome Shielded Integrin Targeted Probes.

Figure 1

(a) A multifunctional reagent module was first synthesized and attached to a linker-targeting vehicle module via a copperless click reaction, to yield a multifunctional probe. (b) Synthesis of the linker-targeting vehicles bearing RGD or RAD peptides. (c) Synthesis of the multifunctional probes with functional groups of F1= DOTA, F2= CyAL5.5 fluorochrome and F3= 5 kDa PEG. Reaction conditions for a: 1) NH2NH2, DMF; 2) CyAL5.5 Acid/ PyBOP/ DMF/ DIPEA; 3) TFA; b: PEG-5K-NHS, DMSO; c: 5a, cRGD-PEG4-DBCO (3a) or RAD-PEG4-DBCO (3b), DMSO; d: PEG-5K-NHS. For the need of the linker arm for RGD/integrin interactions, see Figure S4. Compounds were greater than 90% pure by RP-HPLC and FPLC (Figure 2d).