Author/Authors :
Lennon، نويسنده , , Ian C. and Ramsden، نويسنده , , James A. and Brear، نويسنده , , Catherine J. and Broady، نويسنده , , Simon D. and Muir، نويسنده , , James C.، نويسنده ,
Abstract :
A synthesis of N-acetylcolchinol, a key intermediate in the synthesis of ZD6126, was developed. The enantiodifferentiating step required the catalytic asymmetric hydrogenation of an enamide. After screening a range of metal and ligand combinations it was found that (S,S)-iPr–FerroTANE Ru(methallyl)2 and [(S,S)-tBuFerroTANE Rh(COD)]BF4 gave both high enantioselectivity (>90% ee) and high catalyst utility (molar S/C = 1000).
