Yuichi Suzuki

Enantioselective synthesis of (2S)-5-{4-[2-(4-fluorophenoxy)ethyl]piperazin-1-yl}-2-isopropyl-2-phenyl-pentanenitrile dihydrochloride (E2050) using enzyme-catalyzed kinetic resolution

Abstract Immobilized lipase ( Pseudomonas sp.)-catalyzed transesterification of ( RS )-4-cyano-4-isopropyl-4-phenyl-1-butanol 4 in vinyl acetate gave ( S )-4-cyano-4-isopropyl-4-phenyl-1-butyl acetate 3a with high enantiomeric excess values and conversions (95–97% ee, 30–47%, E =90–93), leaving the enantiomerically pure ( R )-alcohol 4 (>99% ee) unreacted. As 3a can be efficiently converted to E2050, use of the immobilized lipase should provide an economical route for large-scale synthesis of E2050.

Discovery of Novel Neuronal Voltage-Dependent Calcium Channel Blockers Based on Emopamil Left Hand as a Bioactive Template

A series of novel neuronal voltage-dependent calcium channel (VDCC) blockers, with inhibitory activity at low micromolar and moderate solubility in water, was discovered by constructing and screening a focused library based on emopamil (1) left hand (ELH) as a bioactive template.