A rapid on-bead convergent method
for preparing branched peptides
was reported. Linear peptides were prepared on Dbz resin and ligated
various branched cores, including lysine dendrons and other dendritic
compounds. Alongside microwave irradiation, <1.5 equiv of peptides
is sufficient to afford 50–65% yields of pure branched peptides
without chromatographic purification. Remarkably, the desired compounds
were prepared within hours.
An efficient solid-phase
method has been reported to prepare well-defined
lysine defect dendrimers. Using orthogonally protected lysine residues,
pure G2 to G4 lysine defect dendrimers were prepared with 48–95%
yields within 13 h. Remarkably, high-purity products were collected
via precipitation without further purification steps. This method
was applied to prepare a pair of 4-carboxyphenylboronic acid-decorated
defect dendrimers (
16
and
17
), which possessed
the same number of boronic acids. The binding affinity of
16
, in which the ε-amines of G1 lysine are fractured, for glucose
and sorbitol was 4 times that of
17
. This investigation
indicated the role of allocation and distribution of peripheries for
the dendrimer’s properties and activity.
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