Telek András

Biocatalytic asymmetric synthesis of amines via reductive amination

Budapesti Műszaki és Gazdaságtudományi Egyetem

Oláh György Doktori Iskola (Kémia és Vegyészmérnöki tudományok)

Vértessy G. Beáta

Tasnádi Gábor

társ

PhD

The amino functionality is a privileged structural motif in active pharmaceutical ingredients which is underpinned by the large number of small molecules approved by FDA between 2015 and 2020 containing a chiral amine moiety (J. Med. Chem. 2021, 64, 2339‐2381). The aim of the project is the development of an enzyme panel for the synthesis of pharmaceutically relevant chiral secondary and tertiary amines by primarily using imine reductases and reductive aminases. Enzymes will be derived from screening of available enzyme panels as well as from the exploration of the available sequence space using bioinformatic tools. Candidate enzymes will be produced by an external partner, while biochemical and structural characterization will be carried out in a close collaboration with the group of Dr. Beáta Vértessy (Department of Applied Biotechnology and Food Sciences). Target structures are defined from an industrial perspective, focusing on intermediates which generally allow further functionalization. Accordingly, enzymes will be selected and rationally engineered to enable the coupling of bulky carbonyl and amine compounds being relevant to pharma applications. Selected enzymes and reactions will be optimized for preparative‐scale transformations. Chemical characterization will be carried out at Servier Research Institute, Budapest.

2021-09-01

2025-08-31

abszolutóriumot szerzett

Biocatalytic asymmetric synthesis of amines via reductive amination