手性技术与制药化学国际高峰论坛-周其林院士-手性螺环催化剂助推制药工业.pdf

武汉 2015-3-19 手性螺环催化剂助推制药工业 Qi-Lin Zhou （周其林） 元素有机化学国家重点实验室( 南开大学) State Key Lab of Elemento-org Chem, Nankai University Chirality Widely Exists in Nature Chiral Drugs Play A Critical Role for Human Health ~50% Marketing drugs and 2/3 developing drugs are chiral The Methods for Preparation of Optically Active Compounds Chiral Resolution Chiral Transformation Stoichoimetric Asy. Synthesis Asymmetric Catalysis Chiral Amplification Asymmetric catalysis (chemically and enzymetically) is the most efficient method for the preparation of optically active compounds Very Few Asymmetric Catalytic Hydrogenations Have Been Applied in Industry Statistics for the industrial application of enantioselective catalytic reactions Transformation Production Pilot Bench scale 5 t/y 5t/y 50 k 50 kg Hydrogenation of enamides 1 1 2 6 4 Hydrogenation of C=C-COOR 1 0 3 4 6 and C=C-CH-OH Hydrogenation of other C=C 1 0 1 2 2 Hydrogenation of α- and 2 2