A short and chemoenzymatic synthesis of rotigotine using an IR-36-M5 mutant is reported. Focusing on the residues that directly contact the 2-tetralone moiety, we applied structure-guided semi-rational design to obtain a double-mutant F260W/M147Y, which showed a good isolated yield and S-stereoselectivity >99% toward 2-aminotetralin synthesis. Furthermore, the utility of this biocatalytic protocol was successfully demonstrated in the enantioselective synthesis of rotigotine via enzymatic reductive amination as the key step.

中文翻译：

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IRED 催化还原胺化化学酶法全合成罗替高汀

报道了使用 IR-36-M5 突变体的罗替高汀的简短化学酶合成。针对直接接触2-四氢萘酮部分的残基，我们应用结构引导的半理性设计获得了双突变体F260W/M147Y，其对2-氨基四氢化萘的合成表现出良好的分离产率和>99%的S-立体选择性。此外，该生物催化方案的实用性在通过酶还原胺化作为关键步骤的罗替高汀对映选择性合成中得到了成功证明。