Tetrahydroprotoberberine and protoberberine alkaloids are a group of biologically active natural products with complex molecular scaffolds. Isolation from plants is challenging stereoselective synthetic routes, particularly methylated compounds limited, reducing the potential use these compounds. In this work, we describe chemoenzymatic cascades toward various 13-methyl-tetrahydroprotoberberbin...

Transaminase enzymes have significant potential for the stereoselective synthesis of drugs or drug precursors. Here, starting from one prochiral β-tetralone, a short and efficient chemoenzymatic four agonists serotonin/melatonin receptors been developed. The key step is transamination ketone to produce both enantiomers 8-methoxy-2-aminotetraline in high yields enantiomeric excesses. This was fo...