化学
最后
转氨酶
组合化学
有机化学
立体化学
纳米技术
酶
内科学
医学
材料科学
疾病
银屑病性关节炎
作者
Langyu Tang,Xinjie Yang,Ningning Sun,Guojiao Wu,Yuzhou Wu,Fangrui Zhong
标识
DOI:10.1002/cjoc.202400351
摘要
Comprehensive Summary The implementation of divergent protein engineering on the natural transaminase Vf ‐ω‐TA led to the development of two effective mutants (M2 and M8), enabling the enzymatic synthesis of chiral amine precursors of Rivastigmine and Apremilast, respectively. The evolution of the enzymes was guided by crystal structures and a focused mutagenesis strategy, allowing them to effectively address the challenging ketone substrates with significant steric hindrance. Under the optimized reaction parameters, transamination proceeded smoothly in good conversions and with perfect stereochemical control (> 99% ee ). These processes utilize inexpensive α‐methylbenzylamine as an amine donor and avoid the continuous acetone removal and costly LDH/GDH/NADH systems.
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