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. 2021 Jan 21;60(10):5554–5560. doi: 10.1002/anie.202014239

Figure 4.

Figure 4

Enzymatic selective alkylation of pyrazoles using haloalkanes. v36 and NSA‐synthase (50 μM each) was used as catalyst. The reactions were performed with 2 mM pyrazole (3) as substrate, 10 equiv. of haloalkane and 30 °C (iodo‐, bromoethane and iodopropane) as well as 37 °C (iodomethane). The reaction time was 30 h using iodomethane, 40 h in the iodomethane preparative scale reaction, 72 h in using haloethanes and 50 h with 1‐iodopropane. *This reaction was performed on preparative scale (1.0 mmol), please see SI for details. Regioselectivity is described as regioisomeric ratio (r.r.).