C—H Activation, a New Strategy for Synthesis of 3-Substituted Phthalides

Abstract

Phthalides are an important class of compounds owing to their role as the key structural motifs in bioactive natural products and pharmaceutical synthesis. C-H activation has become a promising strategy for preparation of phthalides due to its advantages of high efficiency and atomic economy compared with the traditional methods. In this paper, we summarized recent advances on synthesis of 3-substituted phthalides via C-H activation according to different transition metal catalytic systems.

Synthesis and Antioxidant/Anti-Inflammatory Activity of 3-Arylphthalides

“…The important role of phthalides, both in total synthesis and pharmaceutical chemistry, has attracted attention of chemists and several synthetic strategies have been developed [ 1 , 3 , 27 , 28 , 29 ]. The strategies first described were based preferentially on three synthetic aspects: the construction of the γ-lactone on a six carbon cycle, the construction of the benzene system on a pre-existing γ-lactone, or the concomitant formation of both rings, the benzene and the γ-lactone rings [ 3 ].…”

“…The strategies first described were based preferentially on three synthetic aspects: the construction of the γ-lactone on a six carbon cycle, the construction of the benzene system on a pre-existing γ-lactone, or the concomitant formation of both rings, the benzene and the γ-lactone rings [ 3 ]. More recently, other strategies have been developed, searching either one-pot multicomponent reaction (MCRs) versions as powerful tools for the rapid assembly of molecules [ 30 ] or innovative C–H bond functionalization using simple and unactivated starting materials with the achievement of atom economy and molecular diversity [ 29 ].…”