The robustness of the method for coupling bulky substituents was confirmed by coupling hemin to NH2β-CD via the carboxylate functionality to produce a dark red solid in 71 % yield. Successful synthesis of Compound 15 was confirmed using ESI-MS. However, due to the iron complexed in heme, it is not possible to characterize by NMR; therefore Compound 16 was synthesized using protoporphyrin IX. The synthesis of β-CD conjugated to protoporphyrin IX has been previously published. However, it is on the primary face and involves an arduous synthetic procedure, with unreported final yields . Using the method reported here, yields of 68 % were achieved with a one pot strategy, without any need for chromatographic purification.