Table 2. Enzyme-Catalyzed Hydrolytic Deprotection of the Methyl Ester of (2RS)-4.
| enzymea | time (h)b | product yields (%)c |
|---|---|---|
| PLE | 1.0 | (2RS)-5 (97), 1 (3), (2RS)-4 (ndd) |
| CALB | 0.50 | (2RS)-5 (99), 1 (ndd), (2RS)-4 (ndd) |
| Chirazyme L-5 CA | 1.5 | (2RS)-5 (17), 1 (ndd), (2RS)-4 (83) |
| 3.0 | (2RS)-5 (29), 1 (ndd), (2RS)-4 (71) | |
| Chirazyme L-2 CB | 1.0 | (2RS)-5 (99), 1 (ndd), (2RS)-4 (ndd) |
Enzyme concentration was 1.0 mg/mL. Initial concentration of (2RS)-4 was 1.0 mM in 20 mM sodium citrate buffer (pH 5.0) containing 10% (v/v) DMSO.
Incubation time at 40 °C.
Yields based on HPLC analysis.
nd = not detected.
