title: Synthesis of diverse 4,5-dihydro-3(2H)-pyridazinones on Wang resin.
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 gamma-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.
authors.affiliation: UPRES-Synthèse et extraction de molécules à visée thérapeutique-Faculté de Pharmacie 2, Rennes, France.
authors.forename: N
authors.initials: N
authors.lastname: Gouault
authors.forename: J F
authors.initials: JF
authors.lastname: Cupif
authors.forename: S
authors.initials: S
authors.lastname: Picard
authors.forename: A
authors.initials: A
authors.lastname: Lecat
authors.forename: M
authors.initials: M
authors.lastname: David
mesh_terms: D002087:Butyrates / Q000138:chemical synthesis; D006834:Hydrazines / Q000138:chemical synthesis; D006835:Hydrazones / Q000138:chemical synthesis; D011724:Pyridazines / Q000138:chemical synthesis*; D012116:Resins, Plant / Q000138:chemical synthesis*
chemical_list: D002087:Butyrates; D006834:Hydrazines; D006835:Hydrazones; D011724:Pyridazines; D012116:Resins, Plant