An efficient synthesis of original bis-β-cyclodextrin-[2]cryptorotaxanes in moderate to high yields is described. A synthetic approach based on the template-directed self-assembly threading process in aqueous medium gives a structure stabilized exclusively through non-covalent interactions. This procedure reveals a simple and efficient way to prepare highly organized supramolecular receptors from carefully designed subunits.
![Graphical abstract: Expeditious synthesis of bis-β-cyclodextrinyl-diazacrown-[2]cryptorotaxanes](http://hg.y866.cn/compound/lib/scimg/usr/1/C1CC16171G.jpg)