Gamma Secretase Inhibitor Enzymatic Synthesis of -5,5,5-Trifluoronorvaline

Escherichia coli expressing O (R)-amino acid dehydrogenase 

Gamma secretase inhibitor enzymatic synthesis (R)-5,5,5-trifiuoro-norvaiine. 

Tachykinins are biologically active neuropeptide hormones that are widely distributed throughout the nervous system and implicated in a variety of biological processes such as pain transmission, inflammation, vasodilatation, and secretion [61], The nonpeptide NK-receptor antagonists are potentially useful in the treatment of a variety of chronic diseases including asthma, bronchospasm, arthritis, and migraine [62]. 

The reaction was carried out using immobilized lipase B at 100 g/1 substrate input and 20 g/1 immobilized enzyme input. A reaction )deld of 97% and an ee of 99% were obtained for the desired (S)-monoester 33 [63]. TTie process was scaled up to produce 200 kg of product with an 80% overall isolated 5deld. 

NK1/NK2 dual antagonists enzymatic desymmetrization of diethyl 3-[3, 4 -dichlorophenyl] glutarate. 

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