A facile and efficient preparation of pyrazoloquinolin-4-ones, as potential ligands for the estrogen receptor, via a PIFA [phenyliodine(III)bis(trifluoroacetate)] promoted cyclization reaction with overall yields up to 29% over six steps is described. The employed strategy, based on an electrophilic amidation reaction as the key step of the synthesis, allows the generation of a diverse array of derivatives. © 2008 Elsevier Ltd. All rights reserved.

PIFA-mediated synthesis of novel pyrazoloquinolin-4-ones as potential ligands for the estrogen receptor / M.S. Christodoulou, K.M. Kasiotis, N. Fokialakis, I. Tellitu, S.A. Haroutounian. - In: TETRAHEDRON LETTERS. - ISSN 0040-4039. - 49:50(2008), pp. 7100-7102.

PIFA-mediated synthesis of novel pyrazoloquinolin-4-ones as potential ligands for the estrogen receptor

M.S. Christodoulou;
2008

Abstract

A facile and efficient preparation of pyrazoloquinolin-4-ones, as potential ligands for the estrogen receptor, via a PIFA [phenyliodine(III)bis(trifluoroacetate)] promoted cyclization reaction with overall yields up to 29% over six steps is described. The employed strategy, based on an electrophilic amidation reaction as the key step of the synthesis, allows the generation of a diverse array of derivatives. © 2008 Elsevier Ltd. All rights reserved.
Estrogen receptor; PIFA; Pyrazole; Quinolin-4-ones; Biochemistry; Organic Chemistry; Drug Discovery3003 Pharmaceutical Science
Settore CHIM/06 - Chimica Organica
Settore CHIM/08 - Chimica Farmaceutica
2008
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/495921
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