Sterically bulky metalloporphyrin-catalyzed diastereoselective epoxidation of allyl-substituted alkenes

ORGN 365

Man-Kin Wong, mkwong@hkusua.hku.hk, Wing-Kei Chan, and Chi-Ming Che, cmche@hku.hk. Chemistry Department & Open Lab of Chemical Biology of the Institute of Molecular Technology for Drug Discovery and Synthesis, The University of Hong Kong, Pokfulam Road, Hong Kong SAR, China
Metalloporphyrin-catalyzed alkene epoxidation has been a subject of extensive studies for decades. By judicious modification of the macrocyclic ligand, steric and electronic properties of metalloporphyrin catalysts can be fine-tuned for stereo- and enantioselective alkene epoxidations. Epoxides of allyl-substituted alkenes are versatile synthetic intermediates for organic synthesis. Significant successes have been achieved in cis-selective epoxidation of cyclic allylic alcohols through hydrogen bonding. However, for epoxidation of alkenes without syn-directing group, anti-epoxides would be obtained as major product, and such anti-selectivities are generally poor. Here, we reported that highly diastereoselective epoxidations of allyl-substituted alkenes including allylic alcohols, esters, and amines can be achieved by using sterically bulky metalloporphyrins [Mn(TDCPP)Cl] and [Ru(TDCPP)CO] as catalysts. Our epoxidation protocols afforded anti-epoxides selectively in good yields (up to 99%) with up to >99:1 anti-selectivity. The synthetic utilities of this epoxidation method are highlighted, and transition-state geometries are proposed to rationalize the diastereoselective epoxidation reaction.