THIO ARYLATION OF ACTIVE METHYLENE COMPOUNDS: PREPARATION OF α-THIOARYL-𝛽-DICARBONYLS

Abstract

In recent years, chemistry of organosulfur has gotten noteworthy significant in organic synthesis because sulfur has a vital role in both field pharmaceutical and environmental [1]. The compounds bearing sulfur functionalities are indispensable building blocks in synthetic organic chemistry. Alkyl aryl sulfides and their derivatives are tremendously useful intermediates among all the sulfur compounds in materials science for the synthesis of heterocyclic compounds having both biological and pharmaceutical properties [2,3]. Numerous drugs with an aryl sulfide unit as their core structure are enlisted to treat malarial, Alzheimer’s, Parkinson’s, cancer and HIV diseases [4-7]. A lot of pharmaceutically beneficial heterocyclic molecules such as pyrazoles, oxazoles, and diazepines etc. harness β-diketones as valuable building blocks. Further, α-substituted unsymmetrical β-diketones are significant precursors for producing new quarternary chiral centres. For the formation of carbon sulfur bond between active methylene compounds and thiophenols, one of them needs to be changed to the concordant electrophile. C–S bond present in some biologically vital compounds are represented in figure 1.