酶促化学合成司来吉兰：一种亚胺还原酶催化方法。
Chemoenzymatic Synthesis of Selegiline: An Imine Reductase-Catalyzed Approach.
机构信息
College of Bioscience and Bioengineering, Jiangxi Agricultural University, Nanchang 330045, China.
Tianjin Institute of Industrial Biotechnology, Chinese Academy of Sciences, Tianjin 300308, China.
出版信息
Molecules. 2024 Mar 16;29(6):1328. doi: 10.3390/molecules29061328.
()-Homobenzylic amines are key structural motifs present in ()-selegiline, a drug indicated for the treatment of early-stage Parkinson's disease. Herein, we report a new short chemoenzymatic approach (in 2 steps) towards the synthesis of ()-selegiline via stereoselective biocatalytic reductive amination as the key step. The imine reductase IR36-M5 mutant showed high conversion (97%) and stereoselectivity (97%) toward the phenylacetone and propargyl amine substrates, offering valuable biocatalysts for synthesizing alkylated homobenzylic amines.
()-苯甲基胺是司来吉兰（一种用于治疗早期帕金森病的药物）中的关键结构基序。在此，我们报告了一种新的短化学酶法（分两步）合成（）-司来吉兰的方法，其中立体选择性生物催化还原胺化为关键步骤。亚胺还原酶 IR36-M5 突变体对苯乙酮和炔丙胺底物表现出高转化率（97%）和立体选择性（97%），为合成烷基化的苯甲基胺提供了有价值的生物催化剂。
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