Journal of the American Chemical Society
Communication
sides, rather than inequivalent faces. Such [2]catenanes are
commonly found in the literature.12,13 They are generally
considered to be achiral because they possess a mirror plane
when the mirror planes of the individual rings are brought to
coincide. Yet, moving the rings on either side of the mirror plane
generates axially chiral co-conformations.14,15 These co-
conformations may be either left-handed (M) or right-handed
(P), depending on the relative orientation of the rings. In
contrast with the situation presented in Figure 1a, the motion of
the rings now results in the interconversion of the enantiomeric
co-conformers.16,17 This behavior is somewhat reminiscent of
atropisomerism.11 If the motion of the rings is unconstrained,
which is typically the case in previous reports, the individual co-
conformers interconvert too rapidly to be detected and the
[2]catenane displays no sign of chirality. Here we show that the
chiral co-conformers can become observable when the motion
of the rings is hindered. More importantly, we show that the
dynamic nature of this system can be exploited to easily amplify a
single enantiomer in response to a chemical stimulus.18
Tandem mass spectrometry (Figure S4)21 rapidly confirmed
that [2]catenane 3 was composed of two identical macrocycles,
each resulting from the condensation of one dialdehyde 1 (in
gray) and one dihydrazide 2 (in green).
Attempts to obtain single crystals of 3·4CF3CO2 from
aqueous solutions were unsuccessful. Fortunately, slow vapor
diffusion of isopropyl ether in a concentrated acetonitrile
solution of the hexafluorophosphate salt 3·4PF6 (prepared by
following an anion exchange protocol described in the SI),
yielded single crystals suitable for X-ray diffraction. [2]Catenane
3 is a particularly compact structure. The optimum packing of
the aromatic units results in a decrease of solvent accessible
surface area of ca. 37% compared to that of two non-interlocked
macrocycles, explaining the high yield of the [2]catenane
assembly. The cavity of the individual rings is narrow, oblong,
and delimited by large aromatic walls. Steric demands impose
considerable constraint on the relative orientation of the rings,
which can only be interlocked if the quinoliniums stack as
depicted in Figure 2b. The [2]catenane is thus locked into a
well-expressed axially chiral state. Of all the possible co-
conformers, only the enantiomers (M)-3 and (P)-3 are present
and alternate in the three dimensions of the crystal lattice
(Figure 3).
A sterically hindered [2]catenane composed of rings with
inequivalent sides was assembled following a dynamic
combinatorial approach (Figure 2).19 In water, amphiphilic
Figure 3. Crystal packing showing the alternation between (M)-3 (in
red) and (P)-3 (in blue). Hydrogens and counterions are omitted for
clarity.
Figure 2. (a) Synthesis of [2]catenane 3 from dialdehyde 1 (in gray)
and dihydrazide 2 (in green). The HPLC chromatogram shows the
purity of the crude mixture at the end of the reaction. (b) Crystal
structure of the enantiomers (M)-3 and (P)-3. The acylhydrazone
linkages are colored in yellow. Hydrogens are omitted for clarity.
1
The H NMR spectrum of 3·4CF3CO2 in D2O (Figure 4a)
comprises sharp, well-dispersed resonances, and it does not
significantly change between 278 and 338 K (Figure S5). These
features confirm that [2]catenane 3 has little conformational
freedom. The spectrum is consistent with the C2-symmetrical
structure observed in the solid state. The two rings are
equivalent, and all the protons of an individual ring are
inequivalent.
building blocks frequently self-assemble into catenanes to
minimize the overall hydrophobic surface area in contact with
the environment.13,20 Quinolinium-based dialdehyde 1 (1 mM)
and dihydrazide 2 (1 mM) were solubilized in water at pH 5.
The solution was stirred overnight at 70 °C, allowing for the
reversible formation of acylhydrazone linkages between the
building blocks. On the following day, HPLC analysis disclosed
the near-quantitative conversion of the starting materials into
[2]catenane 3, which was isolated by semipreparative HPLC as a
trifluoroacetate salt (3·4CF3CO2) in 83% yield.
The protons of the inner quinoliniums, buried in the stack, are
substantially upfield-shifted compared to those of the outer
quinoliniums. Moreover, the methylene protons are diaster-
eotopic. In conclusion, the [2]catenane also exists as a racemic
mixture of (M)-3 and (P)-3 in solution. The spectrum shows no
evidence of any other co-conformers.
B
J. Am. Chem. Soc. XXXX, XXX, XXX−XXX