Synthesis and neuroleptic activity of some trans-(2-aminomethyl)-cyclopentyl aryl ketones

Asymmetric Hydrogenation of Tetrasubstituted α,β-Unsaturated Ketones: Access to Chiral 2-Substituted Cyclopentyl Aryl Ketones

“…Chiral cyclopentanes bearing two contiguous stereogenic centers are widely found in natural products and biologically active molecules and are also important building blocks, − in which chiral 2-substituted cyclopentyl aryl ketones are important members (Figure a). − For example, compound A has potential neuroleptic activity, and compound B is a selective diacyl glycerolacyltransferase-1 inhibitor. , Erteberel is an ERβ agonist developed by Eli Lily and Company, and its synthesis is derived from 2-arylcyclopentyl aryl ketone . However, examples for the efficient synthesis of chiral 2-substituted cyclopentyl aryl ketone are relatively rare, − and most of the reported methods suffer from low stereoselectivities and yields or require chiral starting materials and multiple steps.…”

“…5−7 For example, compound A has potential neuroleptic activity, and compound B is a selective diacyl glycerolacyltransferase-1 inhibitor. 5,6 Erteberel is an ERβ agonist developed by Eli Lily and Company, and its synthesis is derived from 2-arylcyclopentyl aryl ketone. 7 However, examples for the efficient synthesis of chiral 2-substituted cyclopentyl aryl ketone are relatively rare, 7−10 and most of the reported methods suffer from low stereoselectivities and yields or require chiral starting materials and multiple steps.…”