
164
Methods of Non-α-Amino Acid Synthesis, Second Edition
2. BH
3
3. CrO
3
-Py
4. LiCH
2
CO
2
Et
5. HPLC-SiO
2
EtOAc
238
CO
2
H
NH
2
NHBoc
CO
2
OH
240
CO
2
H
NH
2
CO
2
H
OH
57%
239
Bestatin (244) is another important statine analog, and it has been shown to be a
competitive inhibitor of aminopeptidase B and of leucine aminopeptidase.
228
Bestatin
is a dipeptide mimetic and a potent inhibitor of the malarial PfA-M1 metallo-amino-
peptidase. The Plasmodium falciparum malarial M1 alanyl-aminopeptidase (PfA-
M1) is an enzyme involved in the terminal stages of hemoglobin digestion and the
generation of an amino acid pool within the parasite. It was prepared from the N