Ring‐Opening Amino Esterification of Cyclic Ketones to Access Distal Amino Acid Derivatives

Abstract

AbstractThis study developed a method of synthesizing distal amino acid derivatives by the ring‐opening reaction of cyclic ketones, following the amino esterification functionalization of both terminals. To achieve this goal, we performed the ring‐opening reaction of cyclic ketones with an aminating reagent and alcohol under metal‐ and photocatalysis‐free conditions in a single step. The method directly afforded distal amino acid derivatives bearing C4−C6, C8, and C12 carbon main chains, such as γ, δ, and ϵ‐amino esters. The obtained amino esters were simply transformed into amino acids by hydrolysis.