Table 1.
Comparison of activities (TTN) and enantioselectivies of purified P450 and P411 variants with azide 1 at 0.1 mol% catalyst loading giving sulfonamide 2 and benzosultam 3. Reaction conditions described in supporting information. TTNs and enantioselectivies determined by HPLC analysis.
| In vitro catalyst | TTN[a] | % ee[b] |
|---|---|---|
| P450BM3 | 2.1 | nd |
| P450BM3-T268A | 15 | 36 |
| P411BM3 | 32 | 20 |
| P411BM3-T268A | 120 | 58 |
| P411BM3-CIS | 310 | 67 |
| P411BM3-CIS-A268T | 82 | 47 |
| P411BM3-CIS-T438S | 383 | 73 |
TTN = total turnover number
(S−R)/(S+R).
nd = not determined.