4.5 Article

An efficient, simple and expedition synthesis of 1-amidoalkyl-2-naphthols as 'drug like' molecules for biological screening

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 18, Issue 2, Pages 788-792

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.11.035

Keywords

amidoalkyl naphthol; ferric hydrogensulfate; multi-component reaction; aminomethyl naphthol; drug like; biologic compound

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An efficient and direct protocol for the preparation of amidoalkyl naphthols employing a multi-component, one-pot condensation reaction of P-naphthol, aromatic aldehydes and acetamide in the presence of ferric hydrogensulfate under solvent, solvent-free and microwave conditions is described. The thermal solvent-free and microwave green procedures offer advantages such as shorter reaction times, simple work-up, excellent yield, recovery and reusability of catalyst. It is noteworthy that 1-amidomethyl-2-naphthols can be converted into important biological 'drug like' active 1-aminomethyl-2-naphthols derivatives by amide hydrolysis. (c) 2007 Elsevier Ltd. All rights reserved.

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