Issue 3, 2012

One-pot synthesis of useful heterocycles in medicinal chemistry using a cascade strategy

Abstract

To access useful heterocycles in medicinal chemistry such as pyridazinones, dihydropyrimidinones, and dihydropyrimidinthiones, a “green” mild and highly efficient one-pot triple cascade was developed involving a Claisen–decarboxylation, electrophilic reaction, and subsequent heterocyclization. In addition, indazoles and benzofurans could also be constructed via a double cascade. To develop the cascade process, a direct Claisen–decarboxylation reaction was firstly optimized. This reaction can then couple with electrophilic reactions including alkylation, Michael addition or aldol reaction to enable the preparation of various aryl ketones in a one-pot fashion.

Graphical abstract: One-pot synthesis of useful heterocycles in medicinal chemistry using a cascade strategy

Supplementary files

Article information

Article type
Communication
Submitted
15 Nov 2011
Accepted
13 Dec 2011
First published
12 Jan 2012

Green Chem., 2012,14, 580-585

One-pot synthesis of useful heterocycles in medicinal chemistry using a cascade strategy

G. Wu, W. Yin, H. C. Shen and Y. Huang, Green Chem., 2012, 14, 580 DOI: 10.1039/C2GC16457D

To request permission to reproduce material from this article, please go to the Copyright Clearance Center request page.

If you are an author contributing to an RSC publication, you do not need to request permission provided correct acknowledgement is given.

If you are the author of this article, you do not need to request permission to reproduce figures and diagrams provided correct acknowledgement is given. If you want to reproduce the whole article in a third-party publication (excluding your thesis/dissertation for which permission is not required) please go to the Copyright Clearance Center request page.

Read more about how to correctly acknowledge RSC content.

Social activity

Spotlight

Advertisements