Solvent-Free and Self-Catalyzed Three-Component Synthesis of Diversely Substituted Pyrazolo[1,4]thiazepinones of Potential Antitumor Activity

ISSN: 1875-6271 (Online)
ISSN: 1570-1794 (Print)


Volume 11, 6 Issues, 2014


Download PDF Flyer




Current Organic Synthesis

Aims & ScopeAbstracted/Indexed in

Ranking and Category:
  • 29th of 57 in Chemistry, Organic

Submit Abstracts Online Submit Manuscripts Online

Editor-in-Chief:
Prof. Eduardo A Castro
Universidad Nacional de La Plata
Buenos Aires
Argentina


View Full Editorial Board

Subscribe Purchase Articles Order Reprints

Current: 2.038
5 - Year: 2.914

Solvent-Free and Self-Catalyzed Three-Component Synthesis of Diversely Substituted Pyrazolo[1,4]thiazepinones of Potential Antitumor Activity

Author(s): Rodrigo Abonia

Affiliation: Department of Chemistry, Universidad del Valle, A. A. 25360, Cali, Colombia.

Abstract

In this work we report the highly efficient solvent-free and self-catalyzed three-component approach for the synthesis of pyrazolo[ 3,4-e][1,4]thiazepin-7(4H)-ones. The reaction between 5-aminopyrazoles, benzaldehydes and mercaptoacetic acid, acting both as reagent and catalyst, at 120 °C lead to the sequential formation of three new single bonds and the release of water as unique by-product, which demonstrates this to be an environmentally friendly three-component procedure. Selected products were evaluated by the NCI (USA) for their antitumor activity. Compound 16b displayed the most remarkable activity against different strains of human tumor cell lines with several GI50 values less than 1.0

Keywords: 5-Aminopyrazoles, mercaptoacetic acid, benzaldehydes, three-component reactions, pyrazolothiazepinones, antitumor activity

Purchase Online Rights and Permissions

Article Details

Volume: 11
First Page: 1
Last Page: 14
Page Count: 14
DOI: 10.2174/1570179411666140327002045
Advertisement

Related Journals




Webmaster Contact: urooj@benthamscience.org Copyright © 2014 Bentham Science