Abstract
Oxazole compounds, including one nitrogen atom and one oxygen atom in a five-membered heterocyclic ring, are present in various biological activities. Due to binding with a widespread spectrum of receptors and enzymes easily in biological systems through various non-covalent interactions, oxazole-based molecules are becoming a kind of significant heterocyclic nucleus, which have received attention from researchers globally, leading them to synthesize diverse oxazole derivatives. The van Leusen reaction, based on tosylmethylisocyanides (TosMICs), is one of the most appropriate strategies to prepare oxazole-based medicinal compounds. In this review, we summarize the recent advances of the synthesis of oxazole-containing molecules utilizing the van Leusen oxazole synthesis from 1972, aiming to look for potential oxazole-based medicinal compounds, which are valuable information for drug discovery and synthesis.
Highlights
The oxazole ring, with one nitrogen atom and one oxygen atom, which are widely displayed in natural products and synthetic molecules, is known as a prime skeleton for drug discovery
A precursor a one-pot reaction mild condition, which is known as the van Leusen oxazoleoxazole synthesis
Shown in Scheme precursor was obtained under the van Leusen oxazole synthesis condition with
Summary
The oxazole ring, with one nitrogen atom and one oxygen atom, which are widely displayed in natural products and synthetic molecules, is known as a prime skeleton for drug discovery. TosMIC a precursor a one-pot reaction mild condition, which is known as the van Leusen oxazoleoxazole synthesis TosMICs under oxazole through a two-step [3+2] cycloaddition reaction from aldehydes with TosMICs under aa base base condition In this process, the TosMIC contains reactive isocyanide carbons, active methylene, and leaving groups as C2N1 “3-atom synthon”. The van Leusen oxazole synthesis allows the preparation of 5- substituted oxazole through a two-step [3+2] cycloaddition reaction from aldehydes with TosMICs under a base oxazole through two-stepthe cycloaddition aldehydes with active. After adding the deprotonated to the aldehyde condition In this process, the TosMIC contains reactive isocyanide carbons, active methylene, and leaving groups as to the aldehyde and bond formation between thesynthon”.
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