Synthesis and Enantioselective Recognition of Chiral Macrocycles with Abundant Binding Sites

Chiral macrocycles R/S-C with abundant recognition sites were synthesized via a simple four-step reaction procedure. These homochiral macrocycles can be easily purified by silica gel column chromatography without the demand for chiral separation. Their structures have been carefully characterized using X-ray crystallography and NMR spectroscopy. R/S-C exhibits enantioselective recognition toward a class of chiral drug intermediates, with an enantioselectivity reaching up to 9.6.