Synthesis of diverse 4,5-dihydro-3(2H)-pyridazinones on Wang resin-Reference-Cited by-同舟云学术

Synthesis of diverse 4,5-dihydro-3(2H)-pyridazinones on Wang resin

Published:2001-07 Issue:7 Volume:53 Page:981-985
ISSN:0022-3573
Container-title:Journal of Pharmacy and Pharmacology
language:en
Short-container-title:

Author:

Gouault N¹,Cupif J F¹,Picard S¹,Lecat A¹,David M¹

Affiliation:

1. U.P.R.E.S. -Synthèse et extraction de molécules à visée thérapeutique - Faculté de Pharmacie, 2 Avenue du professeur Léon Bernard, 35043 Rennes, Cedex, France

Abstract

Abstract An efficient solid-phase synthesis of structurally diverse 4,5-dihydro-3(2H)-pyridazinones is described using readily available substituted 4-oxo-butanoic acids. Polymer-supported γ-keto-esters prepared from Wang resin reacted with several hydrazines to afford the corresponding hydrazones. A protocol developed in mild conditions without isolating the intermediate hydrazone led to pyridazinones in good yields after a cyclization cleavage approach. This successful strategy represents an attractive method for a rapid synthesis of heterocyclic libraries for biological evaluation.

Publisher

Oxford University Press (OUP)

Subject

Pharmaceutical Science,Pharmacology

Link

http://academic.oup.com/jpp/article-pdf/53/7/981/36783175/0022357011776225.pdf

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