We describe the synthesis of a highly water-soluble cryptophane 1 that can be seen as a universal platform for the construction of (129)Xe magnetic resonance imaging (MRI)-based biosensors. Compound 1 is easily functionalized by Huisgen cycloaddition and exhibits excellent xenon-encapsulation properties. In addition, 1 is nontoxic at the concentrations typically used for hyperpolarized (129)Xe MRI.
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