(R)-Selective ω-transaminases are valuable biocatalysts for the synthesis of chiral amines and pharmaceutical intermediates, but their practical application is often limited by insufficient catalytic efficiency, poor operational stability and unfavorable reaction equilibrium. Here, an Actinomycete-derived (R)-selective...
The biocatalytic asymmetric amination of bulky N-heterocyclic ketones is often limited by low enzyme activity and poor performance at high substrate loading. Herein, we developed an efficient (R)-selective transaminase for the synthesis of (R)-1-Boc-3-aminopiperidine through an integrated strategy combining phylogeny-g...
The direct asymmetric synthesis of chiral amides remains a focal point in green manufacturing, particularly for (S)-2-aminobutyramide whose traditional production is often hampered by low atom economy and arduous chiral resolution steps. Here, we report the creation of a non-native bio-amidation activity in Escherichia...
(R)–4-(1H-indol-3-yl)butan-2-amine ((R)-4IBA), encompassing a nitrogen heterocycle and a chiral primary amino group, is a highly appealing precursor in the pharmaceutical domain. The direct amination of the readily available prochiral ketone 4-(1H-indol-3-yl)butan-2-one (4IBO) catalyzed by amine dehydrogenases (AmDHs...
A method for the synthesis of diethyl 4-(1-aryl-3-(ethoxycarbonyl)-1H-pyrazol-4-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylates was developed via a modified Hantzsch three-component cyclocondensation. High structural similarity to known lead antitubercular agents was found using Tanimoto coefficients. In silico...
Quinoxaline-based heterocycles are of interest as potential cholinesterase inhibitors, and this study evaluated a substituted 1-phenyl-[1,2,4]triazolo[4,3-a]quinoxalin-4(5H)-one series against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). The objective was to synthesise and characterise derivatives with...
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