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A New Synthetic Approach to Indazoles Synthesis

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Mon, 2014-07-07 08:45 — Abdel Naser Zaid
Journal Title, Volume, Page: 
Synthesis ; 1997(10): 1140-1142
Year of Publication: 
1997
Link: 
https://www.thieme-connect.com/products/ejournals/abstract/10.1055/s-1997-1328
Authors: 
A. N. Zaid
Dipartimento di Scienze Farmaceutiche, Via Fossato di Mortara 17/19, I-44100, Ferrara, Italy
Current Affiliation: 
Department of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National University, Nablus, Palestine
[email protected]
Pier Giovanni Baraldi
Dipartimento di Scienze Farmaceutiche, Via Fossato di Mortara 17/19, I-44100, Ferrara, Italy, Fax +39(532)29112965
Barbara Cacciari
Dipartimento di Scienze Farmaceutiche, Via Fossato di Mortara 17/19, I-44100, Ferrara, Italy
Giampiero Spalluto
Dipartimento di Scienze Farmaceutiche, Via Fossato di Mortara 17/19, I-44100, Ferrara, Italy
Romeo Romagnoli
Dipartimento di Scienze Farmaceutiche, Via Fossato di Mortara 17/19, I-44100, Ferrara, Italy
Giovanni Braccioli
Dipartimento di Scienze Farmaceutiche, Via Fossato di Mortara 17/19, I-44100, Ferrara, Italy
Maria J. Pineda de las Infantas
Departamento de Química Orgànica y Farmacéutica, Facultad de Farmacía, Campus de Cartuja s/n, 18071 Granada, Spain
Preferred Abstract (Original): 

Stobbe condensation of 3-alkyl- or aryl-4-formylpyrazoles 3a-f with diethyl succinate in the presence of potassium t-butoxide, followed by intramolecular ring closure (Ac2O-NaOAc), afforded the corresponding indazole derivatives 5a-f in 65-85% overall yield. These compounds are good starting materials for transformation to biologically active molecules, such as new pyrazole analogs of the left-hand segment of the potent natural antineoplastic agent CC-1065.