Table 3 Best LEH variants of libraries C and D as catalysts in the hydrolytic desymmetrization of epoxide 1 with formation of (R,R)- or (S,S)-2
Library | Code | Mutations | Favored enantiomer | ee % | c % |
|---|---|---|---|---|---|
C | WT | (S,S) | 2 | 99 | |
SZ57 | I80 V/L114 V | (R,R) | 75 | 99 | |
SZ197 | I80 V | (R,R) | 72 | 93 | |
SZ503 | I80 V/V83I/L114 V | (R,R) | 80 | 97 | |
SIF01 | I80F/V83I/L114 V | (R,R) | 72 | 94 | |
SZ501 | I80F/V83I/L114 V/I116G | (S,S) | 97 | 98 | |
SZ502 | I80F/V83I/L114 V/I116 V | (S,S) | 98 | 95 | |
SZ504 | I80F/V83I/L114I/I116 V | (S,S) | 95 | 98 | |
SZ546 | L114 V/I116 V | (S,S) | 68 | 95 | |
D | TOQ-PA-197-04 | L103I/F134L | (R,R) | 40 | 51 |
TOQ-PA-197-06 | L74F/L103I/F134L | (R,R) | 55 | 35 | |
TOQ-PA-197-01 | L35 V/L74F/L103 V | (S,S) | 36 | 92 | |
TOQ-PA-197-05 | L35 V/L74F | (S,S) | 38 | 67 | |
TOQ-PA-197-07 | L35A/L74F/L103I | (S,S) | 38 | 62 |